
Description | AM095isanantagoNISToftheLPAtype1receptorwithIC50valuesof0.98and0.73μMforrecombinanthumanandmouseLPA1,respectively. | |
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Targets |
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Invitro | AM095isapotentLPA1receptorantagonistbecauseitinhibitedGTPγSbindingtoChinesehamsterovary(CHO)cellmembranesoverexpressingrecombinanthumanormouseLPA1withIC50valuesof0.98and0.73μM,respectively,andexhibitednoLPA1agonism.Infunctionalassays,AM095inhibitedLPA-drivenchemotaxisofCHOcellsoverexpressingmouseLPA1(IC50=778nM)andhumanA2058melanomacells(IC50=233nM)[1]. | |
Invivo | AM095hashighoralbioavailABIlityandamoderatehalf-lifeandiswelltoleratedatthedosestestedinratsanddogsafteroralandintravenousdosing.Itdose-dependentlyreduceSLPA-stimulatedhistaminerelease,attenuatedbleomycin-inducedincreasesincollagen,protein,andinflammatorycellinfiltrationinbronchalveolarlavagefluid,anddecreaseskidneyfibrosisinamouseunilateralureteralobstructionmodel.Despiteitsantifibroticactivity,AM095hasnoeffectonnormalwoundhealingafterincisionalandexcisionalwoundinginrats[1]. |
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