Vorapaxar-SCH-530348-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEVorapaxarCat.No.:HY-10119CASNo.:618385-01-6Synonyms:SCH530348分?式:C??H??FN?O?分?量:492.58作?靶點:ProteaseActivatedReceptor(PAR)作?通路:GPCR/GProtein儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:25mg/mL(50.75mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.0301mL10.1506mL20.3013mL5mM0.4060mL2.0301mL4.0603mL10mM0.2030mL1.0151mL2.0301mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(5.08mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.08mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.08mM);ClearsolutionBIOLOGICALACTIVITY?物活性Vorapaxar(SCH530348)，抗??板藥物，?種選擇性、?服活性和競爭性的凝?酶受體蛋?酶激活受體(PAR-1)拮抗劑，Ki值為8.1nM。Vorapaxar(SCH530348)劑量依賴性抑制凝?酶受體激活肽(TRAP)誘導(dǎo)的??板聚集。IC50&TargetKi:8.1nM(PAR-1)[1]體外研究Vorapaxar(SCH530348)showspotentinhibitionofthrombin-inducedplateletaggregationwithanIC50of47nMandhaTRAP-inducedplateletaggregationwithanIC50of25nM.Vorapaxar(SCH530348)inhibitsthrombininducedcalciumtransientinhumancoronaryarterysmoothmusclecells(HCASMC)withaKiof1.1nM.Italsoinhibitsthrombin-stimulatedthymidineincorporationinHCASMCwithaKiof13nM[1].戶使?本產(chǎn)品發(fā)表的科研?獻?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.Forrese