Betrixaban-hydrochloride-PRT054021-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBetrixabanhydrochlorideCat.No.:HY-10268BCASNo.:2099719-47-6Synonyms:PRT054021hydrochloride分⼦式:C₂₃H₂₃Cl₂N₅O₃分⼦量:488.37作⽤靶点:FactorXa作⽤通路:MetabolicEnzyme/Protease储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Betrixaban(PRT054021)hydrochloride⼀种有效的，具有⼝服活性的选择性factorXa(fXa)抑制剂，IC50为1.5nM。Betrixabanhydrochloride具有抗⾎栓形成效果。IC50&TargetIC50:1.5nM(fXa)[1]Ki:0.117nM(fXa),1.8μM(hERG)[1]体外研究Betrixaban(PRT054021)showsIC50of8.9μMinpatchclamphERGassays[1].BetrixabanshowsanIC50andaKiof6.3μMand3.5μMfortheplasmakallikrein,respectively[1].Betrixaban(hERGKi1.8μM)exhibitssignificantlylowerhERGactivitythanalltheothers(hERGKi⩽0.5μM)[1].Betrixaban(5-25ng/mL)inhibitsthrombingeneration[3].体内研究Betrixaban(0.5mg/kg,i.v.;2.5mg/kg,p.o.)hasbioavailabilityof51.6%indog[1].Betrixaban(0.75mg/kg,i.v.;7.5mg/kg,p.o.)hasbioavailabilityof58.7%inmonkey[1].Betrixabanmediatedwhole-bloodINRincreaseisreversedbyr-Antidote.Afteri.v.infusionfor30min,thetotalplasmaconcentrationsofBetrixabanis0.2±0.01μM,andthepercentagesofunboundinhibitoris40%±7.2%.Afteradministrationofr-Antidote,thetotalplasmaconcentrationincreasedto2.0±0.4μM,andthepercentageofunboundinhibitordeclinedto0.3%±0.1%[2].Betrixaban(3mg/kg)showsnearlycomparableinhibitionofthrombusmasstoenoxaparin1.6mg/kg(76%vs96%inhibition)intherabbitabdominalvenacavamodelofclotaccretiononcottonthreads[3].Betrixaban(19.1mg/kg)isatleastaseffectiveatmaintainingpatencyasenoxaparin7.6mg/kgand1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEclopidogrel3mg/kg/d(90%vs70%vs80%patency,respectively)intheferricchlorideinjurymodelofrodentcarotidartery[3].户使⽤本产品发表的科研⽂献•ThrombHaemost.2018Jul;118(7):1203-1214.•IntJLabHematol.2019Apr;41(2):250-261.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ZhangP,etal.DiscoveryofBetrixaban(PRT054021),N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide,ahighlypotent,selective,andorallyefficaciousfactorXainhibitor.BioorgMedChemLett.2009Apr15;19(8):21[2].LuG,etal.AspecificantidoteforreversalofanticoagulationbydirectandindirectinhibitorsofcoagulationfactorXa.NatMed.2013Apr;19(4):446-51.[3].ChanNC,etal.Profileofbetrixabananditspotentialinthepreventionandtreatmentofvenousthromboembolism.VascHealthRiskManag.2015Jun26;11:343-51.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalappli