I-287-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEI-287Cat.No.:HY-148016CASNo.:2014368-93-3分⼦式:C₃₀H₃₀ClFN₄O₄分⼦量:565.04作⽤靶点:ProteaseActivatedReceptor(PAR);ERK作⽤通路:GPCR/GProtein;MAPK/ERKPathway;StemCell/Wnt储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性I-287⼀种具有⼝服活性的PAR2的选择性抑制剂，对Gαq和Gα12/13活性及其下游效应物起负异构调节作⽤。I-287可减轻CompleteFreund'sadjuvant(HY-153808)诱导的⼩⿏炎症，可⽤于免疫炎症研究。IC50&TargetERK1ERK2体外研究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.体内研究I-287(50mg/kgforp.o.)reducesCompleteFreund'sadjuvant(HY-153808)-inducedinflammationinC57BL/6Jmice[1].AnimalModel:CFA-inducedpawinflammationinadultmaleC57BL/6Jmice[1]1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师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