Vorapaxar-sulfate-SCH-530348-sulfate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEVorapaxarsulfateCat.No.:HY-10119ACASNo.:705260-08-8Synonyms:SCH530348sulfate分⼦式:C₂₉H₃₅FN₂O₈S分⼦量:590.66作⽤靶点:ProteaseActivatedReceptor(PAR)作⽤通路:GPCR/GProtein储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:125mg/mL(211.63mM;Needultrasonic)H2O:<0.1mg/mL(ultrasonic;warming;heatto60°C)(insoluble)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.6930mL8.4651mL16.9302mL5mM0.3386mL1.6930mL3.3860mL10mM0.1693mL0.8465mL1.6930mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(3.52mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.52mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Vorapaxarsulfate(SCH530348sulfate)，抗⾎⼩板药物，⼀种选择性、⼝服活性和竞争性的凝⾎酶受体蛋⽩酶激活受体(PAR-1)拮抗剂，Ki值为8.1nM。Vorapaxarsulfate剂量依赖性抑制凝⾎酶受体激活肽(TRAP)诱导的⾎⼩板聚集。IC50&TargetKi:8.1nM(PAR-1)[1]体外研究Vorapaxarsulfate(SCH530348sulfate)showspotentinhibitionofthrombin-inducedplateletaggregationwithanIC50of47nMandhaTRAP-inducedplateletaggregationwithanIC50of25nM.Vorapaxarsulfate(SCH530348sulfate)inhibitsthrombininducedcalciumtransientinhumancoronaryarterysmoothmusclecells(HCASMC)withaKiof1.1nM.Italsoinhibitsthrombin-stimulatedthymidineincorporationinHCASMCwithaKiof13nM[1].户使⽤本产品发表的科研⽂献•CellDeathDis.2020Jul9;11(7):520.•JMedChem.2017Aug24;60(16):7166-7185.•MolMedRep.2019Jun;19(6):5291-5300.•BiomedResInt.2022Sep20;2022:8265898.•EurJOralSci.2019Aug;127(4):287-293.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].KhoufacheK,etal.PAR1contributestoinfluenzaAviruspathogenicityinmice.JClinInvest.2013Jan;123(1):206-14.[2].KehindeO,etal.Vorapaxar:Anovelagenttobeconsideredinthesecondarypreventionofmyocardialinfarction.JPharmBioalliedSci.2016Apr-Jun;8(2):98-105.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.For