H3R-antagonist-1-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEH3Rantagonist1Cat.No.:HY-112219CASNo.:1448422-61-4分⼦式:C₁₉H₂₃N₃O₃分⼦量:341.4作⽤靶点:HistamineReceptor作⽤通路:GPCR/GProtein;Immunology/Inflammation;NeuronalSignaling储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.溶解性数据体外实验DMSO:100mg/mL(292.91mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.9291mL14.6456mL29.2912mL5mM0.5858mL2.9291mL5.8582mL10mM0.2929mL1.4646mL2.9291mLBIOLOGICALACTIVITY⽣物活性H3R-IN-1⼀种有效的组胺受体3(H3R)反向激动剂，详细信息请参考专利⽂献WO2013107336A1中的化合物2。IC50&TargetHistaminereceptor3[1]体外研究TreatmentwithH3R-IN-1,whichisaH3Rinverseagonist,promotesoligodendrocyteprecursorcell(OPC)differentiationinadose-dependentmanner,atEC50=25nM.Westernblotrevealsasignificantincreaseinexpressionlevelsoftwomarkersofmatureoligodendrocytes,myelin-associatedglycoprotein(MAG)andmyelinebasicprotein(MBP)indifferentiatingoligodendrocytesaftertreatmentwithH3R-IN-1,whichsuggeststhattreatmentwithH3R-IN-1drivesmoreOPCstodifferentiate.H3R-IN-1increasestheForskolin-1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEstimulatedcAMPlevelintheprimaryoligodendrocyteprecursorcellsinadose-dependentmanner[1].体内研究TheabilityofH3R-IN-1toenhanceinvivoremyelinationisdeterminedwiththeCuprizone/Rapamycin-induceddemyelinationmodel.MicearetreatedwithCuprizonedietcombinedwithintraperitonealinjectionsofRapamycinfor5weeksfollowedby9daysofcompoundadministration.CuprizonedietplusintraperitonealinjectionsofRapamycininducedseveredemyelinationinbothcorpuscallosumandcortexandtreatmentwithH3R-IN-1(30mg/kg,9days)significantlyincreasesdensityofmyelinspecificBlack-goldIIstaininginthelesionofcorpuscallosumandcortexinforebrain,comparedtovehiclecontrolgroup[1].PROTOCOLAnimalMice[1]Administration[1]TheC57BL/6miceatageof8weeksarefedwithpowdermousefoodmixedfreshlywith0.2%Cuprizone(w/w)andreceivedailyintraperitonealinjectionofRapamycin(10mg/kgbodyweight)for5weekstoinducedemyelination,thenanimalsareallowedtorecover(removalofCuprizonefromthedietandRapamycininjection)andadministratedwithH3R-IN-1,at30mg/kgbodyweightorally,b.i.d.foranadditional9dayspriortosacrifice.Thebrainsamplesarecollectedforpathologicanalysis[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].WANG,Rong,etal.THERAPEUTICUSES.WO2013107336A1.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplica