Vorapaxar-sulfate-SCH-530348-sulfate-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEVorapaxarsulfateCat.No.:HY-10119ACASNo.:705260-08-8Synonyms:SCH530348sulfate分?式:C??H??FN?O?S分?量:590.66作?靶點(diǎn):ProteaseActivatedReceptor(PAR)作?通路:GPCR/GProtein儲(chǔ)存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:125mg/mL(211.63mM;Needultrasonic)H2O:<0.1mg/mL(ultrasonic;warming;heatto60°C)(insoluble)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.6930mL8.4651mL16.9302mL5mM0.3386mL1.6930mL3.3860mL10mM0.1693mL0.8465mL1.6930mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(3.52mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.52mM);ClearsolutionBIOLOGICALACTIVITY?物活性Vorapaxarsulfate(SCH530348sulfate)，抗??板藥物，?種選擇性、?服活性和競(jìng)爭(zhēng)性的凝?酶受體蛋?酶激活受體(PAR-1)拮抗劑，Ki值為8.1nM。Vorapaxarsulfate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Vorapaxarsulfate(SCH530348sulfate)showspotentinhibitionofthrombin-inducedplateletaggregationwithanIC50of47nMandhaTRAP-inducedplateletaggregationwithanIC50of25nM.Vorapaxarsulfate(SCH530348sulfate)inhibitsthrombininducedcalciumtransientinhumancoronaryarterysmoothmusclecells(HCASMC)withaKiof1.1nM.Italsoinhibitsthrombin-stimulatedthymidineincorporationinHCASMCwithaKiof13nM[1].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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