Firibastat-QGC001-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEFiribastatCat.No.:HY-109058CASNo.:648927-86-0Synonyms:QGC001;RB150分⼦式:C₈H₂₀N₂O₆S₄分⼦量:368.51作⽤靶点:Aminopeptidase作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验H2O:33.33mg/mL(90.45mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7136mL13.5682mL27.1363mL5mM0.5427mL2.7136mL5.4273mL10mM0.2714mL1.3568mL2.7136mL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。-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：PBS1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:100mg/mL(271.36mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Firibastat(QGC001)⼀种⼝服活性的EC33前体药物。Firibastat⼀种⾸创的脑氨肽酶A(APA)抑制剂(Ki=200nM)，选择性和特异性地抑制⾼⾎压⼤⿏脑⾎管紧张素II转化为⾎管紧张素III，并降低⾎压。体内研究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: