Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemERAGE406RCat.No.:HY-178926CASNo.:3034560-21-6分子式:C??H??N?O?分子量:412.48作用靶點(diǎn):CCR;TNFReceptor;InterleukinRelated作用通路:GPCR/GProtein;Immunology/Inflammation;Apoptosis儲(chǔ)存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性RAGE406R是一種口服有效的RAGE-DIAPH1相互作用拮抗劑。RAGE406R可與ctRAGE結(jié)合，阻止RAGE-DIAPH1復(fù)合物的形成，并抑制其相互作用。RAGE406R可降低THP1細(xì)胞中CCL2、TNF和IL-6的表達(dá)。RAGE406R可抑制2型糖尿病小鼠的遲發(fā)型超敏反應(yīng)。RAGE406R可用于糖尿病的研究[1]。IC50&TargetIL-6體外研究RAGE406R(8.1nM)inhibitstheactivationofDIAPH1actinpolymerizationactivitybyctRAGEbyantagonizingtheinteractionbetweenctRAGEandDIAPH1[1].RAGE406R(0.1-5.0μM,1h)dose-dependentlyreducestheintracellularproximityofRAGEandDIAPH1.Afteradding0.1μMRAGE406R,theFRETefficiencydecreasesto4.7%;at5.0μM,itdecreasedto1.6%[1].RAGE406R(0.00006-10μM,1.5h)increasestheinhibitionofRAGEligand-stimulatedSMCmigration,withanIC50of2nMinmurineaorticSMCs[1].RAGE406R(10μM,1.5h)significantlyreducestheexpressionofCCL2,TNF,andIL-6inTHP1cells[1].CellMigrationAssay[1]CellLine:PrimarymurineaorticSMCsConcentration:0.00006μM,0.0002μM,0.001μM,0.002μM,0.005μM,0.014μM,0.041μM,0.123μM,0.370μM,1.111μM,3.333μM,10μMIncubationTime:1.5h1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEResult:IncreasedtheinhibitionofRAGEligand-stimulatedSMCmigration,withanIC50of2nMinmurineaorticSMCs.RealTimeqPCR[1]CellLine:THP1cellsConcentration:10μMIncubationTime:1.5hResult:SignificantlyreducedtheexpressionofCCL2,TNF,andIL6inTHP1cells.體內(nèi)研究RAGE406R(5mg/kg,p.o.,twicedailyforatotalof4doses)cansignificantlyinhibitTcell-mediatedinflammatoryresponseswhenadministeredorallyinCF-1mice[1].RAGE406R(5mg/kg,topicalapplication,twicedailyfor8days)acceleratesthehealingofdiabeticwoundsinmiceandhasamorecomprehensiveanti-inflammatoryeffectinmales[1].AnimalModel:CF-1micewereimmunosensitizedbyinjectionofmethylatedbovineserumalbumin(mBSA)(immunogenbeingmBSA+Freund'sincompleteadjuvantemulsion)intotheleftinguinallymphnode.Threeweekslater,aninflammatoryresponsewaselicitedbyinjectionofmBSA(20μg)intothelefthindpawpad[1].Dosage:5mg/kgAdministration:P.o.,twicedaily(12-hourintervals)foratotalof4dosesResult:Inflammationscoresignificantlyreduced.AnimalModel:Full-thickness1cm×1cmexcisionalwoundswerecreatedonthebacksofmaleandfemalemousemodelsofT2D,ob/obmice;woundswerecoveredwithTegadermcleardressing[1].Dosage:5mg/kgAdministration:Topicalapplication,twicedailyfor8daysResult:Significantlypromotedwoundclosure.Inflammationwasreduced,collagendepositionincreased,andepithelialmigrationaccelerated.Inmalemice,theexpressionofCcl2,TNF,andIL-6wassignificantlyreduced;infemalemice,onlyCcl2expressionwassignificantlydecreased,whileTNFandIL-6showednosignificantchanges.REFERENCES2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemETheophallGG,etal.RAGE-mediatedactivationoftheforminDIAPH1andhumanmacrophageinflammationareinhibitedbyasmallmoleculeantagonist.CellChemBiol.2025Oct16;32(10):1221-1234.e8.McePdfHeightCaution:Producthasnotbeen