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Description | RIPA-56isahighly-potent,selective,andmetabolicallystableRIP1(RIPK1)inhibitor. | ||
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Targets |
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Invitro | RIPA-56showsefficientinhibitionofRIP1kinaseactivity,withanIC50of13nM.ItshowednoinhibitionofRIP3kinaseactivityata10µMconcentration.RIPA-56doesnotinhibitIDOactivityataconcentrationof200µM,whichrepresentsanestimated10,000-foldselectivitywindowbasedontheRIP1ADP-Gloactivityof13nM[1]. | ||
Invivo | RIPA-56hasanimpressivePKprofileinmice,witha3.1hhalf-life,22%oralbioavailABIlity(PO),and100%bioavailabilityfromintraperitonealinjection(IP).RIPA-56hasgreatabilityintransportingacrossbloodbrainbarrier.IntheSIRSmicediseasemodel,RIPA-56efficientlyreducedtumornecrosisfactoralpha(TNFα)-inducedmortalityandmulti-organdamage[1]. |