Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEJE-2147Cat.No.:HY-100212CASNo.:186538-00-1Synonyms:AG1776;KNI-764分?式:C??H??N?O?S分?量:575.72作?靶點(diǎn):HIV;HIVProtease作?通路:Anti-infection;MetabolicEnzyme/Protease儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性JE-2147(AG1776)?種有效的?肽蛋?酶(dipeptideprotease)抑制劑，對(duì)HIV-1蛋?酶(HIV-1protease)的Ki為0.33nM。JE-2147能在體外有效抵抗HIV-1、HIV-2、猴免疫缺陷病毒和各種臨床HIV-1病毒株。IC50&TargetIC50:44nM[HIV-1LAI(SI)],24nM[HIV-1Ba-L(SI)],35nM[HIV-1LAI(NSI)],47nM[HIV-2EHO(SI)][1]Ki:0.33nM(HIV-1protease)[2]體外研究JE-2147(0.01-0.05μM;7days;PBMCandMT-2cells)exhibitshighlypotentantiviralactivityagainstHIV-1withIC50sof44nM,24nM,35nMand47nMforHIV-1LAI(SI),HIV-1Ba-L(SI),HIV-1LAI(NSI)andHIV-2EHO(SI),respectively[1].JE-2147iseffectiveagainstthereplicationofHIV-1IIIBinvariouscells(Tcell,Bcell,macrophage,andPBMC)withIC50valuesrangingfrom31to160nMandalsohadantiviralactivityagainstsimianimmunodefidiencyvirusandHIV-2[2].體內(nèi)研究JE-2147exhibitsgoodoralbioavailabilityandplasmapharmacokineticprofilesindogsandrats[2].PharmacokineticParametersofJE-2147inbeagledogsandmaleSprague-Dawleyrats[2].Sprague-DawleyratsBeagledogsi.v.,10mg/kgi.d.,10mg/kgi.v.,25mg/kgp.o.(fed),25mg/kgp.o.(fasted),25mg/kgt1/2β(min)93/94//Cmax(μM)/0.70?±?0.20/4.02?±?0.725.30?±?1.13Tmax(min)/60/9060F(%)/41.6?±?10.7/32.6?±?0.0637.1?±?0.08CL(L/h/kg)//0.88?±?0.09//Vd,ss(L/kg)//1.58//AUC0-24(μM·min)///10091149AnimalModel:BeagledogsandmaleSprague-Dawleyrats[2]1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEDosage:25mg/kgfordogs;10mg/kgforratsAdministration:i.v.andi.d.forrats;i.v.andp.o.fordogs.Result:Exhibitedfavorablepharmacokineticproperties.REFERENCES[1].YoshimuraK,etal.JE-2147:adipeptideproteaseinhibitor(PI)thatpotentlyinhibitsmulti-PI-resistantHIV-1.ProcNatlAcadSciUSA.1999Jul20;96(15):8675-80.[2].MimotoT,etal.Structure-activityrelationshipofsmall-sizedHIVproteaseinhibitorscontainingallophenylnorstatine.JMedChem.1999May20;42(10):1789-802.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchu