| Description | PF429242isknownasaS1PinhibitorwithanIC50of170nM,showingnosignificantinhibitionoftrypsin,elastase,proteinaseK,plasmin,kallikren,factorXIa,thrombin,orfurinatconcentrationsupto100μMandonlymodestinhibitionofurokinase(IC50=50μM)andfactorXa(IC50=100μM). | ||
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| Targets |
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| Invitro | Inculturedhumanliver(Hep-G2)cells,PF-429242preventsproteolyticprocessingandnucleartranslocationofSREBP,reducestheexpressionofkeygenesinvolvedincholesterolsynthesisandfattyacidsynthesis,andinhibitsbothpathwaysintheabsenceofanycytotoxicity[1].TheadditionofPF-429242suppressestheviralpropagationofallSEROtypesofDENVinseveralprimate-derivedcells[2]. | ||
| Invivo | PKdataforPF-429242showthatithadrapidclearance(CL=75ml/min/kg)andpoororalbioavailABIlity(5%)inrats[1]. |
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