Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEI-287Cat.No.:HY-148016CASNo.:2014368-93-3分?式:C??H??ClFN?O?分?量:565.04作?靶點(diǎn):ProteaseActivatedReceptor(PAR);ERK作?通路:GPCR/GProtein;MAPK/ERKPathway;StemCell/Wnt儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性I-287?種具有?服活性的PAR2的選擇性抑制劑，對(duì)Gαq和Gα12/13活性及其下游效應(yīng)物起負(fù)異構(gòu)調(diào)節(jié)作?。I-287可減輕CompleteFreund'sadjuvant(HY-153808)誘導(dǎo)的??炎癥，可?于免疫炎癥研究。IC50&TargetERK1ERK2體外研究I-287(0-60μM;15-30min)inhibitsPAR2-mediatedactivationofGαqandGα12/13butnotGi/oproteinswhilehasnoeffectonPAR2-mediatedrecruitmentofβarrestin2andreceptorinternalization[1].I-287(0-60μM;15-30min)inhibitsPAR2-mediatedERK1/2activationinHEK293cells[1].I-287(10μM;30min)inhibitsPAR2-inducedsecretionofIL-8cytokineinHCT-116andA549cells[1].WesternBlotAnalysis[1]CellLine:HEK-293cellsConcentration:0-60μMIncubationTime:15minResult:InhibitedPAR2-mediatedERK1/2activationinHEK293cells.體內(nèi)研究I-287(50mg/kgforp.o.)reducesCompleteFreund'sadjuvant(HY-153808)-inducedinflammationinC57BL/6Jmice[1].AnimalModel:CFA-inducedpawinflammationinadultmaleC57BL/6Jmice[1]1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEDosage:50mg/kgAdministration:Oralgavage(p.o.)followingtheCFAResult:ReducesCFA-inducedinflammationinC57BL/6JmiceREFERENCES[1].AvetC,et.al.ThePAR2inhibitorI-287selectivelytargetsGαqandGα12/13signalingandhasanti-inflammatoryeffects.CommunBiol.2020Nov27;3(1):719.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021-58