RU_58841_DataSheet_MedChemExpress

Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:BFH772 is a potent oral VEGFR2 inhibitor, which is highly effective at targeting VEGFR2 kinase with an IC 50 value of 3 nM.IC50 & Target: IC50: 2.7±0.9 nM (hVEGFR2), 1.5±0.53 μM (mVEGFR2), 1.7±0.36 μM (hVEGFR1), 1.1±0.29 μM (hVEGFR3)[1]In Vitro: BFH772 is highly selective; apart from inhibiting VEGFR2 at 3 nM IC 50, it also targets B–RAF, RET, and TIE–2, albeit with atleast 40–fold lower potency. BFH772 is inactive (IC 50>10 μM; >2 μM for cKIT) against all other tyrosine specific– andserine/threonine–specific protein kinases tested. BFH772 inhibits VEGFR2 with IC 50 of 4.6±0.6 nM in CHO cells. BFH772 inhibits VEGFR2 with IC 50 of 3 nM in HUVEC cells. BFH772 inhibits the ligand induced autophosphorylation of RET, PDGFR, and KIT kinases,with IC 50 values ranging between 30 and 160 nM. BFH772 is selective (IC 50 values >0.5 μM) against the kinases of EGFR, ERBB2,INS–R, and IGF–1R and against the cytoplasmic BCR–ABL kinase. IC 50 of BFH772 (<0.01 nM, n=2) demonstrates that they abrogated VEGF induced proliferation at remarkably low nM concentrations [1].In Vivo: BFH772 at 3 mg/kg orally dosed once per day potently inhibits melanoma growth (by 54–90% for primary tumor and71–96% for metastasis growth) as depicted by treatment to control ratios. Dose–response curves of BFH772 at 0.3, 1, and 3 mg/kg demonstrate that even at the lowest concentrations, this naphthalene–1–carboxamide inhibits VEGF induced tissue weight and TIE–2 levels but only reaches statistical significance at 1 mg/kg and above [1].PROTOCOL (Extracted from published papers and Only for reference)Kinase Assay:[1]In vitro kinase assay is based on a filter binding assay, using the recombinant GST–fused kinase domainsexpressed in baculovirus and purified over glutathione–sepharose, γ–[33P]ATP as the phosphate donor, and poly(Glu:Tyr 4:1) peptide as the acceptor. Each GST–fused kinase is incubated under optimized buffer conditions [20 mM Tris–HCl buffer (pH 7.5), 1–3 mM MnCl 2, 3–10 mM MgCl 2, 3–8 μg/mL poly(Glu:Tyr 4:1), 0.25 mg/mL polyethylene glycol 20000, 8 μM ATP, 10 μM sodium vanadate, 1mM DTT] and 0.2 μCi γ–33P ATP in a total volume of 30 μL in the presence or absence of a test substance for 10 min at ambient temperature. The reaction is stopped by adding 10 mL of 250 mM EDTA. Using a 384–well filter system, half the volume istransferred onto an Immobilon–polyvinylidene difluoride membrane. The membrane is then washed extensively and dried, and scintillation counting is performed. IC 50s for compounds are calculated by linear regression analysis of the percentage inhibition [1].Cell Assay: BFH772 is dissolved in DMSO (10 mM) and stored, and then diluted with appropriate medium before use [1]. [1]DifferentBa/F3 cell lines rendered IL–3 independent by transduction with various constitutively active tyrosine kinases are grown in RPMI 1640 medium containing 10% fetal calf serum. For maintenance of parental Ba/F3 cells, the medium is additionally supplemented with 10 ng/mL interleukin–3 (IL–3). For proliferation assays, Ba/F3 cells are seeded on 96–well plates in triplicates at 10000 cells per well and incubated with various concentrations of compounds for 72 h followed by quantification of viable cells using a resazurin sodium salt dye reduction readout (commercially known as Alamar Blue assay). IC 50s are determined with the XLFit Excel Add–In using a four–parameter dose response model [1].Animal Administration: BFH772 is prepared in PEG200 100% (Mice)[1].Product Name:BFH772Cat. No.:HY-100419CAS No.:890128-81-1Molecular Formula:C 23H 16F 3N 3O 3Molecular Weight:439.39Target:VEGFR Pathway:Protein Tyrosine Kinase/RTK Solubility:DMSO: 7.75 mg/mLBFH772 is dissolved in N–methyl pyrrolidone/polyethylene glycol200 (30:70, v/v) (Rat)[1].[1]Mice[1]Female FVB mice weighing between 18 and 20 g are housed in groups of six. Porous chambers containing VEGF (2 μg/mL) in 0.5 mL of 0.8% w/v agar (containing heparin, 20 U/mL) are implanted subcutaneously in the flank of the mice (n=6 per group). VEGF induces the growth of vascularized tissue around the chamber. This response is dose–dependent and can be quantified by measuring the weight and TIE–2 levels of the tissue. Mice are treated either orally once daily with compounds or vehicle (PEG200 100%, 5 mL/kg) starting4–6 h before implantation of the chambers and continuing for 4 days. The animals are sacrificed for measurement of the vascularized tissues 24 h after the last dose. Tissue weight is taken and then a lysate prepared for TIE–2 ELISA analysis .Rat[1]Catheters are implanted into the femoral artery and vein of na?ve female rats strain OFA for BFH772, and BAW2881, or in the jugular vein and femoral artery in female Sprague–Dawley rats for compounds 4, 9, and 10. Animals are allowed to recover for 96 h and are housed in single cages with free access to food and water throughout the experiment. Female OFA rats received 2.5 mg/kg ofBAW2881 dissolved in ethanol/dimethylisosorbide/polyethylene glycol400/D5W (10/15/35/40 v/v) or 1 mg/kg of BFH772 dissolved in N–methyl pyrrolidone/polyethylene glycol200 (30:70, v/v) via injection into the femoral vein. D5W is glucose 5%/water (v/v). Oral administration: BAW2881 and BFH772 are formulated as a micronized suspension (dissolved/suspended in 0.5% carboxymethyl cellulose in distilled water) and administered by gavage to female OFA rats to deliver a dose of 25 mg/kg for BAW2881 or 3 mg/kg BFH772 (n=4 rats per group). For compounds 4, 9, and 10, female Sprague–Dawley rats at 8 weeks of age received an intraveno References:[1]. Bold G, et al. A Novel Potent Oral Series of VEGFR2 Inhibitors Abrogate Tumor Growth by Inhibiting Angiogenesis. J Med Chem. 2016 Jan 14;59(1):132–46.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。

Inhibitors, Agonists, Screening LibrariesSafety Data Sheet Revision Date:Nov.-23-2018Print Date:Nov.-23-20181. PRODUCT AND COMPANY IDENTIFICATION1.1 Product identifierProduct name :Gelucire 14/44Catalog No. :HY-Y1892CAS No. :121548-04-71.2 Relevant identified uses of the substance or mixture and uses advised againstIdentified uses :Laboratory chemicals, manufacture of substances.1.3 Details of the supplier of the safety data sheetCompany:MedChemExpress USATel:609-228-6898Fax:609-228-5909E-mail:sales@1.4 Emergency telephone numberEmergency Phone #:609-228-68982. HAZARDS IDENTIFICATION2.1 Classification of the substance or mixtureNot a hazardous substance or mixture.2.2 GHS Label elements, including precautionary statementsNot a hazardous substance or mixture.2.3 Other hazardsNone.3. COMPOSITION/INFORMATION ON INGREDIENTS3.1 SubstancesSynonyms:NoneFormula:N/AMolecular Weight:N/ACAS No. :121548-04-74. FIRST AID MEASURES4.1 Description of first aid measuresEye contactRemove any contact lenses, locate eye-wash station, and flush eyes immediately with large amounts of water. Separate eyelids with fingers to ensure adequate flushing. Promptly call a physician.Skin contactRinse skin thoroughly with large amounts of water. Remove contaminated clothing and shoes and call a physician.InhalationImmediately relocate self or casualty to fresh air. If breathing is difficult, give cardiopulmonary resuscitation (CPR). Avoid mouth-to-mouth resuscitation.IngestionWash out mouth with water; Do NOT induce vomiting; call a physician.4.2 Most important symptoms and effects, both acute and delayedThe most important known symptoms and effects are described in the labelling (see section 2.2).4.3 Indication of any immediate medical attention and special treatment neededTreat symptomatically.5. FIRE FIGHTING MEASURES5.1 Extinguishing mediaSuitable extinguishing mediaUse water spray, dry chemical, foam, and carbon dioxide fire extinguisher.5.2 Special hazards arising from the substance or mixtureDuring combustion, may emit irritant fumes.5.3 Advice for firefightersWear self-contained breathing apparatus and protective clothing.6. ACCIDENTAL RELEASE MEASURES6.1 Personal precautions, protective equipment and emergency proceduresUse full personal protective equipment. Avoid breathing vapors, mist, dust or gas. Ensure adequate ventilation. Evacuate personnel to safe areas.Refer to protective measures listed in sections 8.6.2 Environmental precautionsTry to prevent further leakage or spillage. Keep the product away from drains or water courses.6.3 Methods and materials for containment and cleaning upAbsorb solutions with finely-powdered liquid-binding material (diatomite, universal binders); Decontaminate surfaces and equipment by scrubbing with alcohol; Dispose of contaminated material according to Section 13.7. HANDLING AND STORAGE7.1 Precautions for safe handlingAvoid inhalation, contact with eyes and skin. Avoid dust and aerosol formation. Use only in areas with appropriate exhaust ventilation.7.2 Conditions for safe storage, including any incompatibilitiesKeep container tightly sealed in cool, well-ventilated area. Keep away from direct sunlight and sources of ignition.Recommended storage temperature:Pure form-20°C 3 years4°C 2 yearsIn solvent-80°C 6 months-20°C 1 monthShipping at room temperature if less than 2 weeks.7.3 Specific end use(s)No data available.8. EXPOSURE CONTROLS/PERSONAL PROTECTION8.1 Control parametersComponents with workplace control parametersThis product contains no substances with occupational exposure limit values.8.2 Exposure controlsEngineering controlsEnsure adequate ventilation. Provide accessible safety shower and eye wash station.Personal protective equipmentEye protection Safety goggles with side-shields.Hand protection Protective gloves.Skin and body protection Impervious clothing.Respiratory protection Suitable respirator.Environmental exposure controls Keep the product away from drains, water courses or the soil. Cleanspillages in a safe way as soon as possible.9. PHYSICAL AND CHEMICAL PROPERTIES9.1 Information on basic physical and chemical propertiesAppearance White to off-white (Oil)Odor No data availableOdor threshold No data availablepH No data availableMelting/freezing point No data availableBoiling point/range No data availableFlash point No data availableEvaporation rate No data availableFlammability (solid, gas)No data availableUpper/lower flammability or explosive limits No data availableVapor pressure No data availableVapor density No data availableRelative density No data availableWater Solubility No data availablePartition coefficient No data availableAuto-ignition temperature No data availableDecomposition temperature No data availableViscosity No data availableExplosive properties No data availableOxidizing properties No data available9.2 Other safety informationNo data available.10. STABILITY AND REACTIVITY10.1 ReactivityNo data available.10.2 Chemical stabilityStable under recommended storage conditions.10.3 Possibility of hazardous reactionsNo data available.10.4 Conditions to avoidNo data available.10.5 Incompatible materialsStrong acids/alkalis, strong oxidising/reducing agents.10.6 Hazardous decomposition productsUnder fire conditions, may decompose and emit toxic fumes.Other decomposition products - no data available.11.TOXICOLOGICAL INFORMATION11.1 Information on toxicological effectsAcute toxicityClassified based on available data. For more details, see section 2Skin corrosion/irritationClassified based on available data. For more details, see section 2Serious eye damage/irritationClassified based on available data. For more details, see section 2Respiratory or skin sensitizationClassified based on available data. For more details, see section 2Germ cell mutagenicityClassified based on available data. For more details, see section 2CarcinogenicityIARC: No component of this product present at a level equal to or greater than 0.1% is identified as probable, possible or confirmed human carcinogen by IARC.ACGIH: No component of this product present at a level equal to or greater than 0.1% is identified as a potential or confirmed carcinogen by ACGIH.NTP: No component of this product present at a level equal to or greater than 0.1% is identified as a anticipated or confirmed carcinogen by NTP.OSHA: No component of this product present at a level equal to or greater than 0.1% is identified as a potential or confirmed carcinogen by OSHA.Reproductive toxicityClassified based on available data. For more details, see section 2Specific target organ toxicity - single exposureClassified based on available data. For more details, see section 2Specific target organ toxicity - repeated exposureClassified based on available data. For more details, see section 2Aspiration hazardClassified based on available data. For more details, see section 212. ECOLOGICAL INFORMATION12.1 ToxicityNo data available.12.2 Persistence and degradabilityNo data available.12.3 Bioaccumlative potentialNo data available.12.4 Mobility in soilNo data available.12.5 Results of PBT and vPvB assessmentPBT/vPvB assessment unavailable as chemical safety assessment not required or not conducted.12.6 Other adverse effectsNo data available.13. DISPOSAL CONSIDERATIONS13.1 Waste treatment methodsProductDispose substance in accordance with prevailing country, federal, state and local regulations.Contaminated packagingConduct recycling or disposal in accordance with prevailing country, federal, state and local regulations.14. TRANSPORT INFORMATIONDOT (US)This substance is considered to be non-hazardous for transport.IMDGThis substance is considered to be non-hazardous for transport.IATAThis substance is considered to be non-hazardous for transport.15. REGULATORY INFORMATIONSARA 302 Components:No chemicals in this material are subject to the reporting requirements of SARA Title III, Section 302.SARA 313 Components:This material does not contain any chemical components with known CAS numbers that exceed the threshold (De Minimis) reporting levels established by SARA Title III, Section 313.SARA 311/312 Hazards:No SARA Hazards.Massachusetts Right To Know Components:No components are subject to the Massachusetts Right to Know Act.Pennsylvania Right To Know Components:No components are subject to the Pennsylvania Right to Know Act.New Jersey Right To Know Components:No components are subject to the New Jersey Right to Know Act.California Prop. 65 Components:This product does not contain any chemicals known to State of California to cause cancer, birth defects, or anyother reproductive harm.16. OTHER INFORMATIONCopyright 2018 MedChemExpress. The above information is correct to the best of our present knowledge but does not purport to be all inclusive and should be used only as a guide. The product is for research use only and for experienced personnel. It must only be handled by suitably qualified experienced scientists in appropriately equipped and authorized facilities. The burden of safe use of this material rests entirely with the user. MedChemExpress disclaims all liability for any damage resulting from handling or from contact with this product.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。

Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:CHIR–99021 is a GSK–3α/β inhibitor with IC 50 of 10 nM/6.7 nM; > 500–fold selectivity for GSK–3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases.IC50 & Target: IC50: 10 nM/6.7 nM (GSK–3α/β)[1]In Vitro: CHIR 99021inhibits human GSK–3β with K i values of 9.8 nM [1]. CHIR 99021 is a small organic molecule that inhibits GSK3α and GSK3β by competing for their ATP–binding sites.In vitro kinase assays reveal that CHIR 99021 specifically inhibits GSK3β (IC 50=~5 nM) and GSK3α (IC 50=~10 nM), with little effect on other kinases [2]. In the presence of CHIR–99021 the viability of the ES–D3 cells is reduced by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM and 69.2% at 10 μM CHIR–99021 with an IC 50 of 4.9μM [3].In Vivo: In ZDF rats, a single oral dose of CHIR 99021 (16 mg/kg or 48 mg/kg) rapidly lowers plasma glucose, with a maximal reduction of nearly 150 mg/dl 3–4 h after administration [1]. CHIR99021 (2 mg/kg) given once, 4 h before irradiation, significantly improves survival after 14.5 Gy abdominal irradiation (ABI). CHIR99021 treatment significantly blocks crypt apoptosis andaccumulation of p–H2AX + cells, and improves crypt regeneration and villus height. CHIR99021 treatment increases Lgr5+ cellsurvival by blocking apoptosis, and effectively prevents the reduction of Olfm4, Lgr5 and CD44 as early as 4 h [4].PROTOCOL (Extracted from published papers and Only for reference)Kinase Assay:[2]Kinases are purified from SF9 cells through use of their His or Glu tag. Glu–tagged proteins are purified, and His–tagged proteins are purified. Kinase assays are performed in 96–well plates with appropriate peptide substrates in a 300–μL reaction buffer (variations on 50 mM Tris–HCl, pH 7.5, 10 mM MgCl 2, 1 mM EGTA, 1 mMdithiothreitol, 25 mMβ–glycerophosphate, 1mM NaF, and 0.01% bovine serum albumin). Peptides has K m values from 1 to 100 μM. CHIR 99021 or CHIR GSKIA is added in 3.5μL of Me 2SO, followed by ATP to a final concentration of 1 μM. After incubation, triplicate 100–μL aliquots are transferred to Combiplate 8 plates containing 100 μL/well of 50 μM ATP and 20 mM EDTA. After 1 hour, the wells are rinsed five times with phosphate–buffered saline, filled with 200 μL of scintillation fluid, sealed, and counted in a scintillation counter 30 min later. All of the steps are at room temperature. The percentage of inhibition is calculated as 100×(inhibitor–no enzyme control)/(Me 2SO control–no enzyme control)[2].Cell Assay: CHIR 99021 is dissolved in DMSO and stored, and then diluted with appropriate media before use [3].[3]The viability of the mouse ES cells is determined after exposure to different concentrations of GSK3 inhibitors for three days using the MTT assay.The decrease of MTT activity is a reliable metabolism–based test for quantifying cell viability; this decrease correlates with the loss of cell viability. 2,000 cells are seeded overnight on gelatine–coated 96–well plates in LIF–containing ES cell medium. On the next day the medium is changed to medium devoid of LIF and with reduced serum and supplemented with 0.1–1 μM BIO, or 1–10 μM SB–216763, CHIR–99021 or CHIR–98014. Basal medium without GSK3 inhibitors or DMSO is used as control. All tested conditions are analyzed in triplicates [3].Product Name:CHIR–99021Cat. No.:HY-10182CAS No.:252917-06-9Molecular Formula:C 22H 18Cl 2N 8Molecular Weight:465.34Target:GSK–3; GSK–3; Autophagy Pathway:Stem Cell/Wnt; PI3K/Akt/mTOR; Autophagy Solubility:DMSO: ≥ 5.1 mg/mLAnimal Administration: CHIR 99021 is formulated as solutions in 20 mM citrate–buffered 15% Captisol or as fine suspensions in0.5% carboxymethylcellulose (Rat)[1].CHIR 99021 is prepared in DMSO and diluted (Mice)[4].[1][4]Rat[1]Primary hepatocytes from male Sprague Dawley rats that weighed <140 g are prepared and used 1–3 h after isolation. Aliquotsof 1×106cells in 1 mL of DMEM/F12 medium plus 0.2% BSA and CHIR 99021(orally at 16 or 48 mg/kg) or controls are incubated in 12–well plates on a low–speed shaker for 30 min at 37°C in a CO2–enriched atmosphere, collected by centrifugation and lysed by freeze/thaw in buffer A plus 0.01% NP40; the GS assay is again performed.Mice[4]Mice 6–10 weeks old are used. The PUMA+/+ and PUMA–/– littermates on C57BL/6 background (F10) and Lgr5–EGFP(Lgr5–EGFP–IRES–creERT2) mice are subjected to whole body irradiation (TBI), or abdominal irradiation (ABI). Mice are injected intraperitoneally (i.p.) with 2 mg/kg of CHIR99021 4 h before radiation or 1 mg/kg of SB415286 28 h and 4 h before radiation. Mice are sacrificed to collect small intestines for histology analysis and western blotting. All mice are injected i.p. with 100 mg/kg of BrdU before sacrifice.References:[1]. Ring DB, et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003 Mar;52(3):588–95.[2]. Bennett CN, et al. Regulation of Wnt signaling during adipogenesis. J Biol Chem. 2002 Aug 23;277(34):30998–1004.[3]. Naujok O, et al. Cytotoxicity and activation of the Wnt/beta–catenin pathway in mouse embryonic stem cells treated with four GSK3 inhibitors.BMC Res Notes. 2014 Apr 29;7:273.[4]. Wang X, et al. Pharmacologically blocking p53–dependent apoptosis protects intestinal stem cells and mice from radiation. Sci Rep. 2015 Apr 10;5:8566.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。

Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:BX471 is a potent, selective non–peptide CCR1 antagonist with K i of 1 nM for human CCR1, and exhibits 250–fold selectivity for CCR1over CCR2, CCR5 and CXCR4.IC50 & Target: Ki: 1 nM (human CCR1)In Vitro: BX 471 is a potent functional antagonist based on its ability to inhibit a number of CCR1–mediated effects including Ca 2+mobilization, increase in extracellular acidification rate, CD11b expression, and leukocyte migration. BX 471 demonstrats a greater than 10,000–fold selectivity for CCR1 compared with 28 G–protein–coupled receptors [1]. BX471 is also able to displace 125I–MIP–1α/CCL3 binding to mouse CCR1 in a concentration–dependent manner with a K i of 215±46 nM. Increasingconcentrations of BX471 inhibits the Ca 2+ transients induced by MIP–1α/CCL3 in both human and mouse CCR1 with IC 50 of 5.8±1nM and 198±7 nM, respectively [2]. BX471 (0.1–10 μM) shows a dose–dependent inhibition of RANTES–mediated andshear–resistant adhesion on IL–1β–activated microvascular endothelium in shear flow in isolated blood monocytes. BX471 alsoinhibits the RANTES–mediated adhesion of T lymphocytes to activated endothelium [4].In Vivo: BX 471 (4 mg/kg, p.o. or i.v.) is orally active with a bioavailability of 60% in dogs. Furthermore, BX 471 effectively reduces disease in a rat experimental allergic encephalomyelitis model of multiple sclerosis [1]. BX471 (20 mg/kg, s.c.) reaches peak plasma levels of 9 μM by around 30 minutes, and this rapidly declines to approximately 0.4 μM after 2 hours. From 4 to 8 hours the drug plasma levels drops to 0.1 μM or lower. Mice treated with 20 mg/kg of BX471 for 10 days shows a reduction of interstitial CD45positive leukocytes of approximately 55%. BX471 has a borderline significant effect on the number of CCR5–positive CD8 cells in the peripheral blood. BX471 reduces the amount of FSP1–positive cells by 65% in UUO kidneys as compared with vehicle control [2].Pretreatment witih BX471 reduces macrophage and neutrophil accumulation in kidney after ischemia–reperfusion injury [3]. PROTOCOL (Extracted from published papers and Only for reference)Cell Assay:[4]Briefly, dermal microvascular endothelial cells grown to confluence in Petri dishes are stimulated with IL–1β (10ng/mL) for 12 h followed by pre–incubation with RANTES (10 nM) for 30 min at 37°C just prior to assay. The plates areassembled as the lower wall in a parallel wall flow chamber and mounted on the stage of an Olympus IMT–2 invertedmicroscope with ×20 and ×40 phase–contrast objectives. Isolated human blood monocytes are isolated and resuspended at 5×105 cells/mL in assay buffer (HBSS) containing 10 mM HEPES, pH 7.4 and 0.5% human serum albumin. Shortly before the assay, 1 mM Mg 2+ and 1 mM Ca 2+ are added. The cell suspensions are kept in a heating block at 37°C during the assay and perfused into the flow chamber at a rate of 1.5 dyn/cm 2 for 5 min. For inhibition experiments, monocytes are preincubated with BX471 at different concentrations (0.1–10 μM) or a Me 2SO control for 10 min at 37°C. The number of firmLy adherent cells after 5min is quantitated in multiple fields (at least five per experiment) by analysis of images recorded with a long integration JVC 3CCD video camera and a JVC SR L 900 E video recorder and are expressed as cells/mm 2. The type of adhesion analyzed is restricted to primary, i.e. direct interactions of monocytes with endothelium.Product Name:BX471Cat. No.:HY-12080CAS No.:217645-70-0Molecular Formula:C 21H 24ClFN 4O 3Molecular Weight:434.89Target:CCR; CCR Pathway:Immunology/Inflammation; GPCR/G Protein Solubility:DMSO: ≥ 51 mg/mLAnimal Administration: BX471 is dissolved in a vehicle of 40% aqueous cyclodextrin.[1]Fasted male beagle dogs (n=3 per treatment group) are given BX 471 either by oral gavage or by intravenous injection via the cephalic vein at a dose of 4 mg/kg. The compound is dissolved in a vehicle of 40% aqueous cyclodextrin. Serial blood samples are collected utilizing an in–dwelling catheter in the jugular vein at the indicated time points up to 6 h post–dosing. EDTA is used as an anticoagulant. The samples are centrifuged (1000× g for 10 min at 4°C), and plasma is stored frozen until analyzed for drug levels by HPLC–MS (electrospray mode operated under a positive ion mode). Plasma samples are thawed and denatured by the addition of four parts of ice–cold methanol containing a fixed amount of an internal standard to one part of plasma. The resulting protein precipitate is removed by centrifugation at 5000× g, and the supernatants are analyzed directly. Concurrently plasma calibration standards of BX 471 are prepared over the range of quantification, processed, and analyzed under identical conditions. A FISONS, VG Platform single quadrupole instrument is used in these analyses with an electrospray inlet operated at 3.57 kV. Chromatographic separation is accomplished using a YMC AQ octadecyl silane reversed phase column (4.6×250 mm) following a short isocratic elution method (35% methanol, 65% water containing 0.1% trifluoroacetic acid). The total column flow (1 mL/min) is split post–column to infuse 50 μL/min into the mass spectrometer. The chromatograms are collected over a total run time of 7.5 min/sample following a 50–μL injection on the column. The ions are collected in a single ion positive ionization mode. A calibration curve for quantification is generated by plotting ion current ratios between the internal standard peak and the analyte in the plasma standards over the quantification range. Calculations of percent oral availability is deduced from the area under curve measurements. Pharmacokinetic parameters are calculated using WinNonLin version 3.0. References:[1]. Liang M, et al. Identification and characterization of a potent, selective, and orally active antagonist of the CC chemokine receptor–1. J Biol Chem. 2000 Jun 23;275(25):19000–8.[2]. Anders HJ, et al. A chemokine receptor CCR–1 antagonist reduces renal fibrosis after unilateral ureter ligation. J Clin Invest. 2002 Jan;109(2):251–9.[3]. Furuichi K, et al. Chemokine receptor CCR1 regulates inflammatory cell infiltration after renal ischemia–reperfusion injury. J Immunol. 2008 Dec 15;181(12):8670–6.[4]. Horuk R, et al. A non–peptide functional antagonist of the CCR1 chemokine receptor is effective in rat heart transplant rejection. J Biol Chem. 2001 Feb 9; 276(6):4199–204.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。

=====================================================================Acq. Operator : Li Shan(LCMS-02) Seq. Line : 84Acq. Instrument : HY-LCMS-02 Location : P2-C-05Injection Date : 6/5/2015 4:13:47 PM Inj : 1 Inj Volume : 3.000 µl Acq. Method : D:\AGLIENT 1260\DATA\20150605\20150605 2015-06-05 09-21-31\100-1000MS+3MIN- 1.5_(0.02%FA).M Last changed : 6/5/2015 9:21:31 AM by Li Shan(LCMS-02)Analysis Method : D:\AGLIENT 1260\METHOD\5-80A(RP-HPLC).M Last changed : 6/5/2015 4:55:55 PM by Li Shan(LCMS-02) (modified after loading)Method Info : 10-80A,16MIN Catalog No : HY-12588 Batch#16482 A-RP-132 Additional Info : Peak(s) manually integrated min0.51 1.52 2.53mAU200400600800DAD1 B, Sig=214,4 Ref=off (D:\AGLIENT...60\DATA\20150605\20150605 2015-06-05 09-21-31\BIZ2015-605-DJL9.D)0.394 0.498 2.228 ===================================================================== Area Percent Report ===================================================================== Sorted By : Signal Multiplier : 1.0000Dilution : 1.0000Do not use Multiplier & Dilution Factor with ISTDs Signal 1: DAD1 B, Sig=214,4 Ref=off Peak RetTime Type Width Area Height Area # [min] [min] [mAU*s] [mAU] %----|-------|----|-------|----------|----------|--------| 1 0.394 MM 0.0425 2829.96558 1108.66125 99.2783 2 0.498 MM 0.0339 5.77030 2.83656 0.2024 3 2.228 MM 0.0639 14.80108 3.85942 0.5192 Totals : 2850.53696 1115.35724 ===================================================================== *** End of Report ***=====================================================================Acq. Operator : Li Shan(LCMS-02) Seq. Line : 84Acq. Instrument : HY-LCMS-02 Location : P2-C-05Injection Date : 6/5/2015 4:13:47 PM Inj : 1 Inj Volume : 3.000 µl Acq. Method : D:\AGLIENT 1260\DATA\20150605\20150605 2015-06-05 09-21-31\100-1000MS+3MIN- 1.5_(0.02%FA).M Last changed : 6/5/2015 9:21:31 AM by Li Shan(LCMS-02)Analysis Method : D:\AGLIENT 1260\METHOD\5-80A(RP-HPLC).M Last changed : 6/5/2015 4:56:55 PM by Li Shan(LCMS-02) (modified after loading)Method Info : 10-80A,16MIN Catalog No : HY-12588 Batch#16482 A-RP-132 Additional Info : Peak(s) manually integrated min0.51 1.52 2.530100000200000300000400000500000MSD1 TIC, MS File (D:\AGLIENT 1260\DATA\20150605\20150605 2015-06-05 09-21-31\BIZ2015-605-DJL9.D) ES-API, Pos, Sca0.392MS Signal: MSD1 TIC, MS File, ES-API, Pos, Scan, Frag: 50 Spectra averaged over upper half of peaks. Noise Cutoff: 1000 counts. Reportable Ion Abundance: > 10%. Retention Mol. Weight Time (MS) MS Area or Ion 0.392 2110102 250.10 I 249.10 Im/z 100200300400500600020406080100*MSD1 SPC, time=0.377:0.413 of D:\AGLIENT 1260\DATA\20150605\20150605 2015-06-05 09-21-31\BIZ2015-605-DJL9.D ES-API,Max: 377429251.1 249.1 *** End of Report ***。

Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:AG–1024 (Tyrphostin) inhibits IGF–1R autophosphorylation with IC50 of 7 μM, less potent to IR with IC50 of 57 μM.IC50 value: 7 uM (IGF–1R autophosphorylation); 57 uM (IR) [1]Target: IGF–1R; IRin vitro: AG–1024 blocks the IGF–1 receptor and IR autophosphorylation with IC50 of 7 μM and 57 μM, respectively. AG–1024 also inhibits the receptor tyrosine kinase activity towards exogenous substrates (TKA) with IC50 values of 18 μM and 80 μM, respectively[1]. Human breast cancer cell line MCF–7 exposure to Tyrphostin AG 1024 inhibited proliferation and induced apoptosis in atime–dependent manner, and the degree of growth inhibition for IC20 plus irradiation (4 Gy) was up to 50% compared to the control.Examination of Tyrphostin AG 1024 effects on radiation response demonstrated a marked enhancement in radiosensitivity andamplification of radiation–induced apoptosis [2]. AG–1024 significantly inhibits melanoma cell proliferation with an IC50 of <50 nM in the absence of serum, by blocking MAPK/ERK2 signaling, subsequently rapidly inducing pRb dephosphorylation and activation, and eventually the formation of growth suppressive pRb–E2F complexes [3].in vivo: Administration of AG–1024 at a dose of 30 μg for 10 days significantly inhibits the tumor growth of Ba/F3–p210 xenograft in mice [4].References:[1]. Párrizas M, et al. Specific inhibition of insulin–like growth factor–1 and insulin receptor tyrosine kinase activity and biological function by tyrphostins.Endocrinology. 1997 Apr;138(4):1427–33.[2]. Wen B, et al. Tyrphostin AG 1024 modulates radiosensitivity in human breast cancer cells. Br J Cancer. 2001 Dec 14;85(12):2017–21.[3]. von Willebrand M, et al. The tyrphostin AG1024 accelerates the degradation of phosphorylated forms of retinoblastoma protein (pRb) and restores pRb tumor suppressive function in melanoma cells. Cancer Res. 2003 Mar 15;63(6):1420–9.[4]. Deutsch E, et al. Tyrosine kinase inhibitor AG1024 exerts antileukaemic effects on STI571–resistant Bcr–Abl expressing cells and decreases AKT phosphorylation. Br J Cancer. 2004 Nov 1;91(9):1735–41.Product Name:AG1024Cat. No.:HY-10253CAS No.:65678-07-1Molecular Formula:C 14H 13BrN 2O Molecular Weight:305.17Target:IGF–1R; Autophagy Pathway:Protein Tyrosine Kinase/RTK; Autophagy Solubility:10 mM in DMSOCaution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@ Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。

Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:SNS–032 is a selective inhibitor of cyclin–dependent kinase (CDK), inhibiting CDK2/7/9 with IC 50s of 48 nM/62 nM/4 nM.IC50 & Target: IC50: 48 nM (CDK2), 62 nM (CDK7), 4 nM (CDK9)In Vitro: SNS–032 has low sensitivity to CDK1 and CDK4 with IC 50 of 480 nM and 925 nM, respectively. SNS–032 effectively kills chronic lymphocytic leukemia cells in vitro regardless of prognostic indicators and treatment history. Compared with flavopiridol and roscovitine, SNS–032 is more potent, both in inhibition of RNA synthesis and at induction of apoptosis. SNS–032 activity is readily reversible; removal of SNS–032 reactivates RNA polymerase II, which led to resynthesis of Mcl–1 and cell survival [1].SNS–032 inhibits three dimensional capillary network formations of endothelial cells. SNS–032 completely prevents U87MGcell–mediated capillary formation of HUVECs. In addition, SNS–032 significantly prevents the production of VEGF in both cell lines,SNS–032 prevents in vitro angiogenesis, and this action is attributable to blocking of VEGF. Preclinical studies have shown that SNS–032 induces cell cycle arrest and apoptosis across multiple cell lines [2]. SNS–032 blocks the cell cycle via inhibition of CDKs 2and 7, and transcription via inhibition of CDKs 7 and 9. SNS–032 activity is unaffected by human serum [3]. SNS–032 induces a dose–dependent increase in annexin V staining and caspase–3 activation. At the molecular level, SNS–032 induces a marked dephosphorylation of serine 2 and 5 of RNA polymerase (RNA Pol) II and inhibits the expression of CDK2 and CDK9 anddephosphorylated CDK7[5].In Vivo: SNS–032 (15 mg/kg, i.p.) inhibits both xenografted BaF3–T674I cells and KBM5–T315I cells in vivo. SNS–032 abrogates the growth of tumors transplanted in nude mice with downregulation of T674I PDGFRα and T315I–Bcr–Abl [4].PROTOCOL (Extracted from published papers and Only for reference)Cell Assay:[2]Cell Titer–Glo (CTG) luminescent assay is performed to measure the growth curves of both HUVECs andU87MG cells. U87MG cells and HUVECs (2×103 cells/well) are seeded in a 96–well microplate in a final volume of 100 mL. After 24hours, cells are treated with various doses of SNS–032 (0–0.5 mM) for 24, 48, or 72 hours. After completion of the treatment, 100 mL of CTG solution is added to each well and incubated for 20 minutes at room temperature in the dark. Lysate (50 mL) is transferred to a 96–well white plate, and luminescence is measured by POLARstar OPTIMA. Percent cell growth is calculated by considering 100%growth at the time of SNS–032 addition.Animal Administration: SNS–032 is dissolved in tissue culture grade DMSO. [4]Nude nu/nu BALB/c mice are housed in barrier facilities with a 12–hour light–dark cycle, with food and water available ad libitum. A mixture of 1×107 of BaF3–T674I cells withMatrigel or KBM5–T315I cells (3×107) are inoculated subcutaneously on the flanks of 4– to 6–week–old male nude mice.Tumors are measured every other day with use of calipers. Tumor volumes are calculated by the following formula: a 2×b×0.4,where a is the smallest diameter and b is the diameter perpendicular to a. Four days after subcutaneous inoculation, when tumors are palpable (appr 100 mm 3), mice are randomized to receive treatment with vehicle (tissue culture medium containing DMSO 0.1%v/v) or SNS–032 (15 mg/kg injected intraperitoneally every 2 days) for about 2 weeks. SNS–032 is dissolved in tissue culture gradeProduct Name:SNS–032Cat. No.:HY-10008CAS No.:345627-80-7Molecular Formula:C 17H 24N 4O 2S 2Molecular Weight:380.53Target:CDK Pathway:Cell Cycle/DNA Damage Solubility:10 mM in DMSODMSO before dilution. The body weight, feeding behavior, and motor activity of each animal are monitored as indicators of general health. The animals are then euthanized, and tumor xenografts are immediately removed, weighed, stored, and fixed.References:[1]. Chen R, et al. Mechanism of action of SNS–032, a novel cyclin–dependent kinase inhibitor, in chronic lymphocytic leukemia. Blood. 2009 May 7;113(19):4637–45.[2]. Ali MA, et al. SNS–032 prevents tumor cell–induced angiogenesis by inhibiting vascular endothelial growth factor. Neoplasia. 2007 May;9(5):370–81.[3]. Conroy A, et al. SNS–032 is a potent and selective CDK 2, 7 and 9 inhibitor that drives target modulation in patient samples. Cancer Chemother Pharmacol. 2009 Sep;64(4):723–32.[4]. Wu Y, et al. Cyclin–dependent kinase 7/9 inhibitor SNS–032 abrogates FIP1–like–1 platelet–derived growth factor receptor α and bcr–abl oncogene addiction in malignant hematologic cells.Clin Cancer Res. 2012 Apr 1;18(7):1966–78. Epub 2012 Mar 23.[5]. Walsby E, et al. The cyclin–dependent kinase inhibitor SNS–032 has single agent activity in AML cells and is highly synergistic with cytarabine.Leukemia. 2011 Mar;25(3):411–9. Epub 2011 Jan 7.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。

ST-588PTSA/Fluorescent Polymer DualInline SensorUser ManualOctober12,2020Rev.2.00Pyxis Lab,Inc.1729Majestic Dr.Suite5Lafayette,CO80026USA©2017Pyxis Lab,Inc.Pyxis Lab Proprietary and ConfidentialTable of Contents1Introduction21.1Main Features (2)2Specifications3 3Unpacking Instrument43.1Standard Accessories (4)3.2Optional Accessories (5)4Installation64.1ST-588Piping (6)4.2ST-588SS Piping (6)4.3Wiring (7)4.4Connecting via Bluetooth (8)4.5Connecting via USB (8)5Setup and Calibration with uPyxis®Mobile App95.1Download uPyxis®Mobile App (9)5.2Connecting to uPyxis®Mobile App (9)5.3Calibration Screen and Reading (10)5.4Diagnosis Screen (11)5.5Device Info Screen (12)6Setup and Calibration with uPyxis®Desktop App126.1Install uPyxis®Desktop App (12)6.2Connecting to uPyxis®Desktop App (13)6.3Information Screen (13)6.4Calibration Screen (14)6.5Diagnosis Screen (14)7Outputs157.14–20mA Output Setup (15)7.2Communication using Modbus RTU (15)8Sensor Maintenance and Precaution158.1Methods to Cleaning the ST-588 (16)8.2Storage (16)9Troubleshooting17 10Contact Us18Warranty InformationConfidentialityThe information contained in this manual may be confidential and proprietary and is the property of Pyxis Lab,rmation disclosed herein shall not be used to manufacture,construct,or otherwise reproduce the goods rmation disclosed herein shall not be disclosed to others or made public in any manner without the express written consent of Pyxis Lab,Inc.Standard Limited WarrantyPyxis Lab warrants its products for defects in materials and workmanship.Pyxis Lab will,at its option,repair or replace instrument components that prove to be defective with new or remanufactured components (i.e.,equivalent to new).The warranty set forth is exclusive and no other warranty,whether written or oral, is expressed or implied.Warranty TermThe Pyxis warranty term is thirteen(13)months ex-works.In no event shall the standard limited warranty coverage extend beyond thirteen(13)months from original shipment date.Warranty ServiceDamaged or dysfunctional instruments may be returned to Pyxis for repair or replacement.In some in-stances,replacement instruments may be available for short duration loan or lease.Pyxis warrants that any labor services provided shall conform to the reasonable standards of technical com-petency and performance effective at the time of delivery.All service interventions are to be reviewed and authorized as correct and complete at the completion of the service by a customer representative,or des-ignate.Pyxis warrants these services for30days after the authorization and will correct any qualifying deficiency in labor provided that the labor service deficiency is exactly related to the originating event.No other remedy,other than the provision of labor services,may be applicable.Repair components(parts and materials),but not consumables,provided during a repair,or purchased individually,are warranted for90days ex-works for materials and workmanship.In no event will the in-corporation of a warranted repair component into an instrument extend the whole instrument’s warranty beyond its original term.Warranty ShippingA Repair Authorization(RA)Number must be obtained from Pyxis Technical Support before any product can be returned to the factory.Pyxis will pay freight charges to ship replacement or repaired products to the customer.The customer shall pay freight charges for returning products to Pyxis.Any product returned to the factory without an RA number will be returned to the customer.To receive an RMA you can generate a request on our website at https:///request-tech-support/.Pyxis Technical SupportContact Pyxis Technical Support at+1(866)203-8397,*********************,or by filling out a request for support at https:///request-tech-support/.1IntroductionThe Pyxis ST-588inline fluorometer probe simultaneously measures the concentration of PTSA and Fluores-cent Polymer in water.It can be simply inserted to the compression fitting port of a custom-made tee.The standard ST-001installation tee provided with each ST-588sensor,has two¾inch female NPT ports and can be placed to an existing¾inch sample water line.Pyxis Lab also offers2”and3”Tee formats for larger flow installations.The4–20mA current output of the ST-588probe can be connected to any controller that accepts an isolated or non-isolated4–20mA input.The ST-588probe is a smart device.In addition to mea-suring PTSA and Fluorescent Polymer,the ST-588probe has extra photo-electric components that monitor the color and turbidity of the sample water.This extra feature allows automatic color and turbidity com-pensation to eliminate interference commonly associated with real-world waters.The Pyxis ST-588probe has a short fluidic channel and can be easily cleaned.The fluidic and optical ar-rangement of the ST-588probe is designed to overcome shortcomings associated with other fluorometers that have a distal sensor surface or a long,narrow fluidic cell.Traditional inline fluorometers are susceptible to color and turbidity interference and fouling and are difficult to properly clean.1.1Main FeaturesThe ST-588measures PTSA and Fluorescent Polymer in a water sample and includes the following features:•Easy calibration with using uPyxis®Mobile or Desktop App.•Automatic compensation for turbidity up to150NTU and color created by up to10ppm iron or equivalent to10ppm humic acid.•Diagnostic information(probe fouling,color or turbidity over range,failure modes)are available in uPyxis®App or via Modbus RTU.•Easy to remove from the system for cleaning and calibration without the need for any tools.2SpecificationsTable1.ST-588Specifications*With Pyxis’s continuous improvement policy,these specifications are subject to change without notice.†The fluorescent polymer concentration scale is based on the polymer containing0.25mole%fluorescent monomer.Typical polymer specifications are attached below but may vary by producer.‡See Figure4for ST-588SS dimensions.3Unpacking InstrumentRemove the instrument and accessories from the shipping container and inspect each item for any damage that may have occurred during shipping.Verify that all accessory items are included.If any item is missing or damaged,please contact Pyxis Lab Customer Service at*********************.3.1Standard Accessories•Tee Assembly3/4”NPT(1x Tee,O-ring,and Nut)P/N:ST-001*NOTE*ST-001is not included for ST-588SS•8-Pin Female Adapter/Flying Leads Cable(1.5ft)•User Manual available online at https:///support/3.2Optional AccessoriesFigure1.4Installation4.1ST-588PipingThe provided ST-001Tee Assembly can be connected to a pipe system through the3/4”female ports,either socket or NPT threaded.To properly install the ST-588probe into the ST-001Tee Assembly,follow the steps below:1.Insert the provided O-ring into the O-ring groove on the tee.2.Insert the ST-588probe into the tee.3.Tighten the tee nut onto the tee to form a water-tight,compression seal.Figure2.Dimension of the ST-588and the ST-001Tee Assembly(mm)4.2ST-588SS PipingThe ST-588SS probe has3/4”female NPT threaded ports on the probe itself and therefore does not require a custom tee assembly.It is recommended that two3/4”NPT to1/4”tubing adapters are used to connect the probe to the sampling system.Sample water entering the probe must be cooled down to below104°F (40°C).The probe can be held by a1.75-inch pipe clamp or mounted to a panel with four1/4-28bolts.See Figure4for ST-588SS dimensions.Figure3.Dimension of the ST-588SS(inch)4.3WiringIf the power ground terminal and the negative4–20mA terminal in the controller are internally connected (non-isolated4–20mA input),it is unnecessary to connect the4–20mA negative wire(gray)to the4–20mA negative terminal in the controller.If a separate DC power supply other than that from the controller is used,make sure that the output from the power supply is rated for22–26VDC@85mA.*NOTE*The negative24V power terminal(power ground)and the negative4–20mA ter-minal on the ST-588probe are internally connected.Follow the wiring table below to connect the ST-588probe to a controller:Table2.*Internally connected to the power ground4.4Connecting via BluetoothA Bluetooth adapter(P/N:MA-WB)can be used to connect a ST-588probe to a smart phone with the uPyxis®Mobile App or a computer with the uPyxis®Desktop App.Figure4.Bluetooth connection to ST-588probe4.5Connecting via USBA USB-RS485adapter(P/N:MA-485)can be used to connect a ST-588probe to a computer with the uPyxis®Desktop App.*NOTE*Using non-Pyxis USB-RS485adapters may result in permanent damage of the ST-588probe communication hardware.B connection to ST-588probe5Setup and Calibration with uPyxis®Mobile App5.1Download uPyxis®Mobile AppDownload uPyxis®Mobile App from Apple App Store or Google Play.Figure6.5.2Connecting to uPyxis®Mobile AppTurn on Bluetooth on your mobile phone(Do not pair the phone Bluetooth to the ST-588probe).Open uPyxis®Mobile App.Once the app is open the app will start to search for the sensor.Once the uPyxis®Mobile App connects to the sensor,press the ST-588probe.Figure7.5.3Calibration Screen and ReadingWhen connected,the uPyxis®Mobile App will default to the Calibration screen.From the Calibration screen,you can perform calibrations by pressing on Zero Calibration,Slope Calibration,and4–20mA Span for either Fluorescent Polymer or PTSA,independently.Follow the screen instructions for each calibration step.Figure8.5.4Diagnosis ScreenFrom the Diagnosis screen,you can check the diagnosis condition.This feature may be used for technical support when communicating with*********************.To preform a probe cleaniness check,first select the Diagnosis Condition which defines the fluid type that the ST-588probe in currently measuring,then press Cleanliness Check.If the probe is clean,a Clean mes-sage will be shown.If the probe is severely fouled,a Dirty message will be shown.In this case,follow the procedure in the Methods to Cleaning the ST-588section of this manual.Figure9.5.5Device Info ScreenFrom the Device Info screen.You can name the Device or Product as well as set the Modbus address.Figure10.6Setup and Calibration with uPyxis®Desktop App6.1Install uPyxis®Desktop AppDownload the latest version of uPyxis®Desktop software package from:https:///upyxis/this setup package will download and install the Framework4.5(if not previously installed on the PC),the USB driver for the USB-Bluetooth adapter(MA-NEB),the USB-RS485adapter(MA-485),and the main uPyxis®Desktop application.Double click the uPyxis.Setup.exe file to install.Figure11.Click Install to start the installation process.Follow the screen instructions to complete the USB driver and uPyxis®installation.6.2Connecting to uPyxis®Desktop AppWhen the uPyxis®Desktop App opens,click on Device,then click either Connect via USB-Bluetooth or Connect via USB-RS485depending on the connection type.Figure12.6.3Information ScreenOnce connected to the device,a picture of the device will appear on the top left corner of the window and the uPyxis®Desktop App will default to the Information screen.On the Information screen you can set the information description for Device Name,Product Name,and Modbus Address,then click Apply Settings to save.Figure13.6.4Calibration ScreenTo calibrate the device,click on Calibration.On the Calibration screen there are six calibration options:•Fluorescent Polymer:Zero Calibration,Slope Calibration,and4-20mA Span•PTSA:Zero Calibration,Slope Calibration,and4-20mA SpanThe screen also displays the reading of the device.The reading refresh rate is every4seconds.Figure14.6.5Diagnosis ScreenAfter the device has been calibrated and installation has been completed,to check diagnosis,click on Di-agnosis.When in the Diagnosis screen you can view the Diagnosis Condition of the device.This feature may be used for technical support when communicating with*********************.To preform a probe Cleaniness Check,first select the Diagnosis Condition which defines the fluid type that the ST-588probe inCheck.If the probe is clean,a Clean message will be shown.message will be shown.In this case,follow the procedure in theof this manual.Figure15.7Outputs7.14–20mA Output SetupThe4–20mA output of the ST-588sensor is scaled as:•Fluorescent Polymer:–4mA=0ppm–20mA=20ppm•PTSA:–4mA=0ppb–20mA=200ppb7.2Communication using Modbus RTUThe ST-588probe is configured as a Modbus slave device.In addition to the ppm Fluorescent Polymer and ppb PTSA values,many operational parameters,including warning and error messages,are available via a Modbus RTU connection.Contact Pyxis Lab Customer Service(*********************)for more informa-tion.8Sensor Maintenance and PrecautionThe ST-588probe is designed to provide reliable and continuous Fluorescent Polymer and PTSA readings even when installed in moderately contaminated industrial cooling waters.Although the optics are com-pensated for the effects of moderate fouling,heavy fouling will prevent the light from reaching the sensor, resulting in low readings and the potential for product overfeed if the ST-588probe is used as part of an au-tomated control system.When used to control product dosing,it is suggested that the automation system be configured to provide backup to limit potential product overfeed,for example by limiting pump size or duration,or by alarming if the pumping rate exceeds a desired maximum limit.The ST-588probe is designed to be easily removed,inspected,and cleaned if required.It is suggested that the ST-588probe be checked for fouling and cleaned/calibrated on a monthly basis.Heavily contam-inated waters may require more frequent cleanings.Cleaner water sources with less contamination may not require cleaning for several months.The need to clean the ST-588probe can be determined by the Cleanliness Check using either the uPyxis®Mobile App(see the Mobile Diagnosis Screen section)or the uPyxis®Desktop App(see the Desktop Diagnosis Screen section).8.1Methods to Cleaning the ST-588Any equipment in contact with industrial cooling systems is subject to many potential foulants and con-taminants.Our inline probe cleaning solutions below have been shown to remove most common foulants and contaminants.A small,soft bristle brush,Q-Tips cotton swab,or soft cloth may be used to safely clean the probe housing and the quartz optical sensor channel.These components and more come with a Pyxis Lab Inline Probe Cleaning Solution Kit(P/N:SER-01)which can be purchased at our online Estore/Catalog https:///product/probe-cleaning-kit/Figure16.Inline Probe Cleaning Solution KitTo clean the ST-588probe,soak the lower half of the probe in100mL inline probe cleaning solution for 10minutes.Rinse the ST-588probe with distilled water and then check for the flashing blue light inside the ST-588probe quartz tube.If the surface is not entirely clean,continue to soak the ST-588probe for an e the small,soft bristle brush and Q-Tips cotton swabs as necessary to remove any remaining contaminants in the ST-588probe quartz tube.8.2StorageAvoid long term storage at temperature over100°F.In an outdoor installation,properly shield the ST-588 probe from direct sunlight and precipitation.9TroubleshootingIf the ST-588probe output signal is not stable and fluctuates significantly,make an additional ground con-nection––connect the clear(shield,earth ground)wire to a conductor that contacts the sample water electrically such as a metal pipe adjacent to the ST-588tee.Carry out routine calibration verification against a qualified Fluorescent Polymer and PTSA combined stan-dard.After properly cleaning the ST-588sensor,carry out the zero point calibration with distilled water and slope calibration using the qualified Fluorescent Polymer and PTSA combined standard.10Contact UsPyxis Lab,Inc1729Majestic Dr.Suite5Lafayette,CO80026USAPhone:+1(866)203-8397Email:*********************。

Inhibitors, Agonists, Screening Libraries Data SheetBIOLOGICAL ACTIVITY:Alda–1 is a potent ALDH2 agonist, which significantly improves ALDH2 activity.In Vivo: Alda–1 treatment results in a significant decrease of 4–HNE–protein content in the plasma of apoE -/- mice. Alda–1administration leads to a slight increase in gene expression related to neurogenesis (Nog ), mitochondrial biogenesis (CYTB , ND1),and apoptosis (Bax , Gsk3b ) in the Hp of apoE -/- mice. Alda–1 administration leads to 2 and 10 differentially expressed proteins in theFCx and Hp of apoE -/- mice, respectively [1]. Alda–1 (1.5 mg/kg, b.w., i.p.) administration significantly increases the climbing time,tends to reduce the immobility time and increases the swimming time of the prenatally stressed rats in the forced swim test.Moreover, treatment of prenatally stressed rats with Alda–1 significantly increases number of entries into the open arms of the maze and the time spent therein, as assessed by elevated plus–maze test [2]. Alda–1 (8.5 mg/kg, i.p.) with glucose significantly lowers 4–HNE and FJB–positive cells in the cerebral cortex of Alda–1–treated rats than in DMSO–treated rats 24 h after glucose administration [3]. Alda–1 (10 mg/kg per day) treatment prevents aldehydic overload, mitochondrial dysfunction and improves ventricular function in post–MI cardiomyopathy rats [4].PROTOCOL (Extracted from published papers and Only for reference)Cell Assay:[2]Spleen cells (4×106 cells/mL) are stimulated by optimal concentrations of concanavalin A (Con A; 2.5μg/mL and 0.6 μg/mL) and lipopolysaccharide (LPS, 5 μg/mL) and are incubated in 96–well plates at final volume of 0.2mL for 72 h. Cell proliferation is determined by adding 0.5 μCi of [3H]–thymidine per well at 16 h before the end of the incubation.The cultures are harvested with an automatic cell harvester, and [3H] thymidine incorporation is assessed using a liquid scintillationcounter.Animal Administration: Alda–1 is dissolved in 1 mL/kg b.w. DMSO/water 50/50.[2]After behavioral verification at three months of age,the animals are divided into the following four groups: control, control + Alda–1, prenatally stressed and prenatally stressed + Alda–1(6 animals per group). Alda–1 injections are given intraperitoneally (i.p.) once daily at a dose of 1.5 mg/kg b.w. (dissolved in 1 mL/kg b.w. DMSO/water 50/50) for 14 days. At the same time, the control and prenatally stressed rats receive 1 mL/kg b.w. DMSO/water 50/50. The injections of Alda–1 and vehicle are given between 10 a.m and 11 a.m. In the last five days of Alda–1 treatment the behavioral parameters in the elevated plus maze test and then in the forced swim test are measured.References:[1]. Stachowicz A, et al. Proteomic Analysis of Mitochondria–Enriched Fraction Isolated from the Frontal Cortex and Hippocampus of Apolipoprotein E Knockout Mice Treated with Alda–1, an Activator of Mitochondrial Aldehyde Dehydrogenase (ALDH2). Int J Mol Sci.[2]. Stachowicz A, et al. The impact of mitochondrial aldehyde dehydrogenase (ALDH2) activation by Alda–1 on the behavioral and biochemical disturbances in animal model of depression. Brain Behav Immun. 2016 Jan;51:144–53.Product Name:Alda–1Cat. No.:HY-18936CAS No.:349438-38-6Molecular Formula:C 15H 11Cl 2NO 3Molecular Weight:324.16Target:Aldehyde Dehydrogenase (ALDH)Pathway:Metabolic Enzyme/Protease Solubility:DMSO: ≥ 51 mg/mL[3]. Ikeda T, et al. Effects of Alda–1, an Aldehyde Dehydrogenase–2 Agonist, on Hypoglycemic Neuronal Death. PLoS One. 2015 Jun 17;10(6):e0128844.[4]. Gomes KM, et al. Aldehydic load and aldehyde dehydrogenase 2 profile during the progression of post–myocardial infarction cardiomyopathy: benefits of Alda–1. Int J Cardiol. 2015 Jan 20;179:129–138.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。

Inhibitors, Agonists, Screening LibrariesSafety Data Sheet Revision Date:Jun.-20-2017Print Date:Jun.-20-20171. PRODUCT AND COMPANY IDENTIFICATION1.1 Product identifierProduct name :RU 58841Catalog No. :HY-10561CAS No. :154992-24-21.2 Relevant identified uses of the substance or mixture and uses advised againstIdentified uses :Laboratory chemicals, manufacture of substances.1.3 Details of the supplier of the safety data sheetCompany:MedChemExpress USATel:609-228-6898Fax:609-228-5909E-mail:sales@1.4 Emergency telephone numberEmergency Phone #:609-228-68982. HAZARDS IDENTIFICATION2.1 Classification of the substance or mixtureNot a hazardous substance or mixture.2.2 GHS Label elements, including precautionary statementsNot a hazardous substance or mixture.2.3 Other hazardsNone.3. COMPOSITION/INFORMATION ON INGREDIENTS3.1 SubstancesSynonyms:RU58841; RU–58841Formula:C17H18F3N3O3Molecular Weight:369.34CAS No. :154992-24-24. FIRST AID MEASURES4.1 Description of first aid measuresEye contactRemove any contact lenses, locate eye-wash station, and flush eyes immediately with large amounts of water. Separate eyelids with fingers to ensure adequate flushing. Promptly call a physician.Skin contactRinse skin thoroughly with large amounts of water. Remove contaminated clothing and shoes and call a physician.InhalationImmediately relocate self or casualty to fresh air. If breathing is difficult, give cardiopulmonary resuscitation (CPR). Avoid mouth-to-mouth resuscitation.IngestionWash out mouth with water; Do NOT induce vomiting; call a physician.4.2 Most important symptoms and effects, both acute and delayedThe most important known symptoms and effects are described in the labelling (see section 2.2).4.3 Indication of any immediate medical attention and special treatment neededTreat symptomatically.5. FIRE FIGHTING MEASURES5.1 Extinguishing mediaSuitable extinguishing mediaUse water spray, dry chemical, foam, and carbon dioxide fire extinguisher.5.2 Special hazards arising from the substance or mixtureDuring combustion, may emit irritant fumes.5.3 Advice for firefightersWear self-contained breathing apparatus and protective clothing.6. ACCIDENTAL RELEASE MEASURES6.1 Personal precautions, protective equipment and emergency proceduresUse full personal protective equipment. Avoid breathing vapors, mist, dust or gas. Ensure adequate ventilation. Evacuate personnel to safe areas.Refer to protective measures listed in sections 8.6.2 Environmental precautionsTry to prevent further leakage or spillage. Keep the product away from drains or water courses.6.3 Methods and materials for containment and cleaning upAbsorb solutions with finely-powdered liquid-binding material (diatomite, universal binders); Decontaminate surfaces and equipment by scrubbing with alcohol; Dispose of contaminated material according to Section 13.7. HANDLING AND STORAGE7.1 Precautions for safe handlingAvoid inhalation, contact with eyes and skin. Avoid dust and aerosol formation. Use only in areas with appropriate exhaust ventilation.7.2 Conditions for safe storage, including any incompatibilitiesKeep container tightly sealed in cool, well-ventilated area. Keep away from direct sunlight and sources of ignition.Recommended storage temperature:Powder-20°C 3 years4°C 2 yearsIn solvent-80°C 6 months-20°C 1 monthShipping at room temperature if less than 2 weeks.7.3 Specific end use(s)No data available.8. EXPOSURE CONTROLS/PERSONAL PROTECTION8.1 Control parametersComponents with workplace control parametersThis product contains no substances with occupational exposure limit values.8.2 Exposure controlsEngineering controlsEnsure adequate ventilation. Provide accessible safety shower and eye wash station.Personal protective equipmentEye protection Safety goggles with side-shields.Hand protection Protective gloves.Skin and body protection Impervious clothing.Respiratory protection Suitable respirator.Environmental exposure controls Keep the product away from drains, water courses or the soil. Cleanspillages in a safe way as soon as possible.9. PHYSICAL AND CHEMICAL PROPERTIES9.1 Information on basic physical and chemical propertiesAppearance White to off-white (Solid)Odor No data availableOdor threshold No data availablepH No data availableMelting/freezing point No data availableBoiling point/range No data availableFlash point No data availableEvaporation rate No data availableFlammability (solid, gas)No data availableUpper/lower flammability or explosive limits No data availableVapor pressure No data availableVapor density No data availableRelative density No data availableWater Solubility No data availablePartition coefficient No data availableAuto-ignition temperature No data availableDecomposition temperature No data availableViscosity No data availableExplosive properties No data availableOxidizing properties No data available9.2 Other safety informationNo data available.10. STABILITY AND REACTIVITY10.1 ReactivityNo data available.10.2 Chemical stabilityStable under recommended storage conditions.10.3 Possibility of hazardous reactionsNo data available.10.4 Conditions to avoidNo data available.10.5 Incompatible materialsStrong acids/alkalis, strong oxidising/reducing agents.10.6 Hazardous decomposition productsUnder fire conditions, may decompose and emit toxic fumes.Other decomposition products - no data available.11.TOXICOLOGICAL INFORMATION11.1 Information on toxicological effectsAcute toxicityClassified based on available data. For more details, see section 2Skin corrosion/irritationClassified based on available data. For more details, see section 2Serious eye damage/irritationClassified based on available data. For more details, see section 2Respiratory or skin sensitizationClassified based on available data. For more details, see section 2Germ cell mutagenicityClassified based on available data. For more details, see section 2CarcinogenicityIARC: No component of this product present at a level equal to or greater than 0.1% is identified as probable, possible or confirmed human carcinogen by IARC.ACGIH: No component of this product present at a level equal to or greater than 0.1% is identified as a potential or confirmed carcinogen by ACGIH.NTP: No component of this product present at a level equal to or greater than 0.1% is identified as a anticipated or confirmed carcinogen by NTP.OSHA: No component of this product present at a level equal to or greater than 0.1% is identified as a potential or confirmed carcinogen by OSHA.Reproductive toxicityClassified based on available data. For more details, see section 2Specific target organ toxicity - single exposureClassified based on available data. For more details, see section 2Specific target organ toxicity - repeated exposureClassified based on available data. For more details, see section 2Aspiration hazardClassified based on available data. For more details, see section 212. ECOLOGICAL INFORMATION12.1 ToxicityNo data available.12.2 Persistence and degradabilityNo data available.12.3 Bioaccumlative potentialNo data available.12.4 Mobility in soilNo data available.12.5 Results of PBT and vPvB assessmentPBT/vPvB assessment unavailable as chemical safety assessment not required or not conducted.12.6 Other adverse effectsNo data available.13. DISPOSAL CONSIDERATIONS13.1 Waste treatment methodsProductDispose substance in accordance with prevailing country, federal, state and local regulations.Contaminated packagingConduct recycling or disposal in accordance with prevailing country, federal, state and local regulations.14. TRANSPORT INFORMATIONDOT (US)This substance is considered to be non-hazardous for transport.IMDGThis substance is considered to be non-hazardous for transport.IATAThis substance is considered to be non-hazardous for transport.15. REGULATORY INFORMATIONSARA 302 Components:No chemicals in this material are subject to the reporting requirements of SARA Title III, Section 302.SARA 313 Components:This material does not contain any chemical components with known CAS numbers that exceed the threshold (De Minimis) reporting levels established by SARA Title III, Section 313.SARA 311/312 Hazards:No SARA Hazards.Massachusetts Right To Know Components:No components are subject to the Massachusetts Right to Know Act.Pennsylvania Right To Know Components:No components are subject to the Pennsylvania Right to Know Act.New Jersey Right To Know Components:No components are subject to the New Jersey Right to Know Act.California Prop. 65 Components:This product does not contain any chemicals known to State of California to cause cancer, birth defects, or anyother reproductive harm.16. OTHER INFORMATIONCopyright 2017 MedChemExpress. The above information is correct to the best of our present knowledge but does not purport to be all inclusive and should be used only as a guide. The product is for research use only and for experienced personnel. It must only be handled by suitably qualified experienced scientists in appropriately equipped and authorized facilities. The burden of safe use of this material rests entirely with the user. MedChemExpress disclaims all liability for any damage resulting from handling or from contact with this product.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。