AdipoRon-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAdipoRonhydrochlorideCat.No.:HY-110164CASNo.:1781835-20-8分⼦式:C₂₇H₂₉ClN₂O₃分⼦量:464.98作⽤靶点:AdiponectinReceptor作⽤通路:MetabolicEnzyme/Protease储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性AdipoRonhydrochloride⼀种可⼝服的，特异性的AdipoR激动剂，能够与AdipoR1和AdipoR2结合，Kd值分别为1.8和3.1μM。IC50&TargetKd:1.8μM(AdipoR1),3.1μM(AdipoR2)[1]体外研究AdipoRonhydrochlorideisanorallyactiveandspecificAdipoRagonist,bindstoAdipoR1andAdipoR2,withKdsof1.8and3.1μM.AdipoRon(50nM-50μM)increasesAMPKphosphorylationviaAdipoR1[1].AdipoRon(50μM)dose-dependentlyattenuatestheexpressionofTNF-αandTGF-β1intheL02cells.AdipoRonexhibitssignificantanddosage-dependentgrowthsuppressiononmacrophages[2].AdipoRontreatmentsignificantlyimprovescardiacfunctionalrecoveryafterreperfusion,andinhibitspost-MIapoptosis[3].AdipoRonexertsvasodilationbymechanismsdistincttoadiponectinandinducesvasorelaxationwithoutamarkeddecreaseinVSMC[Ca2+]i[4].体内研究AdipoRon(50ꢀmg/kg,i.v.)cuasessignificantphosphorylationofAMPKinskeletalmuscleandliverofwild-typemicebutnotAdipor1−/−ꢀAdipor2−/−double-knockoutmice[1].AdipoRon(0.02,0.1,and0.5mg/kg,i.g.)alleviatesD-GalNinducedhepatotoxicityinmice,andpreventshepaticarchitecturedistortionagainstD-GalNchallenge.ThehepatoprotectivepotentialofAdipoRonisparticularlyevidentinhigherdosages(0.1and0.5mg/kg)[2].EnhancedcardiomyocyteapoptosisinAPN-deficientmiceisrescuedbyAdipoRon(50mg/kg,p.o.)administration.AntiapoptoticeffectofAdipoRonisattenuatedbutnotlostinAMPK-DNmice[3].PROTOCOL1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellAssay[2]TheeffectsofAdipoRonontheproliferationofparenchymalandnon-parenchymalhepatocytesareevaluatedinvitroviaL02andRAW264.7,byMTTassayasdescribedwithslightmodification:100μLcellssuspension(6×104/mL)areseededina96-wellplateandincubatedfor18h.FreshmediawithAdipoRonareaddedatspecifiedconcentrations,andtheincubationscontinueforafurther24h.Thencellsareincubatedfor4hwith0.5mg/mLofMTT,andanalyzedinamicroplatereaderat490nm.Eachgroupisperformedinsixreplications.Themeanabsorbancevaluescorrectedforablank(mediumonly)arecalculatedaspercentagesofsurvival[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice[2]Administration[2]After3daysofacclimation,micearerandomLydividedintosixgroups(9miceineach):control,model,bicyclol(20mg/kg),AdipoRon(0.02mg/kg,0.1mg/kg,0.5mg/kg).ThesyntheticAdipoRonandbicyclolaredissolvedinDMSOanddilutedbysalinecontaining0.5%sodiumcarboxymethylcellulose(CMC-Na)[finalvehicle:5%DMSO(v/v)salinesolution].Alltestgroupsareadministeredwithvehicle(controlandmodelgroups)ortherapeuticagents(bicyclolorAdipoRongroups)atadosingvolumeof10mL/kg,byintragastric(i.g.)gavagetwiceperdayforthreeconsecutivedayspriortoD-GalNadministration.2hafterlasttreatment,micearechallengedwithasingleintraperitoneal(i.p.)administrationofD-GalNsalinesolutionatadoseof600mg/kgtoinduceacuteliverinjury,whilethecontrolgroupmicereceivesalineinstead.Thenmicearefastedfor20hbeforeorbitalbloodcollection.Finally,allanimalsaresacrificedbycervicaldislocation,andliversareharvestedforbiochemicalorhistopathologyanalysis[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•MolPsychiatry.2020Mar4.•ProgNeurobiol.2021Jul29;102125.•RedoxBiol.August2022,102390.•Diabetes.2021Jun;70(6):1303-1316.•ActaPharmacolSin.2022Aug2.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].Okada-IwabuM,etal.Asmall-moleculeAdipoRagonistfortype2diabetesandshortlifeinobesity.Nature.2013Nov28;503(7477):493-9.[2].WangY,etal.HepatoprotectiveeffectsofAdipoRonagainstd-galactosamine-inducedliverinjuryinmice.EurJPharmSci.2016Aug9;93:123-131.[3].ZhangY,etal.AdipoRon,thefirstorallyactiveadiponectinreceptoractivator,attenuatespostischemicmyocardialapoptosisthroughbothAMPK-mediatedandAMPK-independentsignalings.AmJPhysiolEndocrinolMetab.2015Aug1;309(3):E275-82.[4].HongK,etal.AdiponectinReceptorAgonist,AdipoRon,CausesVasorelaxationPredominantlyViaaDirectSmoothMuscleAction.Microcirculation.2016Apr;23(3):207-20.McePdfHeight2/2MasterofBio