Firibastat-QGC001-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEFiribastatCat.No.:HY-109058CASNo.:648927-86-0Synonyms:QGC001;RB150分?式:C?H??N?O?S?分?量:368.51作?靶點:Aminopeptidase作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗H2O:33.33mg/mL(90.45mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.7136mL13.5682mL27.1363mL5mM0.5427mL2.7136mL5.4273mL10mM0.2714mL1.3568mL2.7136mL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：PBS1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:100mg/mL(271.36mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Firibastat(QGC001)?種?服活性的EC33前體藥物。Firibastat?種?創(chuàng)的腦氨肽酶A(APA)抑制劑(Ki=200nM)，選擇性和特異性地抑制??壓??腦?管緊張素II轉(zhuǎn)化為?管緊張素III，并降低?壓。體內(nèi)研究Whengivenorally,Firibastat(0.1-30mg/kg;p.o.)crossesthegastrointestinalandblood-brainbarriers,entersthebrain,andgeneratestwoactivemoleculesofEC33whichinhibitbrainAPAactivity,blockingbrainangiotensinIIIformation,anddecreasebloodpressureforseveralhoursinhypertensiverats[2].AnimalModel:NormotensiveandhypertensiveDOCA-saltrats[1]Dosage:0.1-30mg/kgAdministration:P.o.Result:Resultinginadose-dependentdecreaseinmeanarterialbloodpressure(MABP).REFERENCES[1].FerdinandKC,etal.EfficacyandSafetyofFiribastat,AFirst-in-ClassBrainAminopeptidaseAInhibitor,inHypertensiveOverweightPatientsofMultipleEthnicOrigins.Circulation.2019;140(2):138-146.[2].KeckM,etal.OrallyActiveAminopeptidaseAInhibitorProdrugs:CurrentStateandFutureDirections.CurrHypertensRep.2019;21(7):50.Published2019May21.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel: