Rosiglitazone-sodium-BRL-49653-sodium-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemERosiglitazonesodiumCat.No.:HY-B0700CASNo.:316371-83-2Synonyms:BRL49653sodium分⼦式:C₁₈H₁₈N₃NaO₃S分⼦量:379.41作⽤靶点:PPAR;TRPChannel;Autophagy作⽤通路:CellCycle/DNADamage;MetabolicEnzyme/Protease;Vitamin

DRelated/NuclearReceptor;MembraneTransporter/Ion

Channel;NeuronalSignaling;Autophagy储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Rosiglitazonesodium⼀种有效的，选择性的PPARγ激活剂，对PPARγ1，PPARγ2和PPARγ的EC50值分别为30nM，100nM和60nM，对PPARγ的Kd值约为40nM；Rosiglitazonesodium同时为TRPchannels的调节剂，可抑制TRPM2,TRPM3的活性，激活TRPC5的活性。IC50&TargetPPARγ1PPARγ230nM(EC50)100nM(EC50)体外研究RosiglitazonesodiumisapotentandselectiveactivatorofPPARγ,withEC50sof30nMand100nMforPPARγ1andPPARγ2,respectively,andaKdofappr40nMforPPARγ.Rosiglitazone(BRL49653,0.1,1,10μM)promotesdifferentiationofC3H10T1/2stemcellstoadipocytes[1].Rosiglitazone(Compound6)activatesPPARγ,withanEC50of60nM[2].Rosiglitazone(1μM)activatesPPARγ,whichbindstoNF-α1promotertoactivategenetranscriptioninneurons.Rosiglitazone(1μM)alsoprotectsNeuro2Acellsandhippocampalneuronsagainstoxidativestress,andup-regulatesBCL-2expressioninanNF-α1-dependentmanner[3].RosiglitazonecompletelyinhibitsTRPM3withIC50valuesof9.5and4.6μMagainstnifedipine-andPregS-evokedactivity,butsucheffectsarenotviaPPARγ.RosiglitazoneinhibitsTRPM2athigherconcentration,withanIC50ofappr22.5μM.RosiglitazoneisastrongstimulatorofTRPC5channels,withanEC50of-30μM[4].体内研究Rosiglitazone(5mg/kg,p.o.)decreasestheserumglucoseindiabeticrats.RosiglitazonealsodecreasesIL-6,TNF-α,andVCAM-1levelsindiabeticgroup.Rosiglitazoneincombinationwithlosartanincreasesglucose1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEcomparedtodiabeticandLos-treatedgroups.RosiglitazonesignificantlyamelioratesendothelialdysfunctionindicatedbyasignificantlylowercontractileresponsetoPEandAngIIandenhancementofACh-provokedrelaxationinaortasisolatedfromdiabeticrats[5].PROTOCOLKinaseAssay[1]cDNAencodingaminoacids174-475ofPPARγ1isamplifiedviapolymerasechainreactionandinsertedintobacterialexpressionvectorpGEX-2T.GST-PPARγLBDisexpressedinBL21(DE3)plysScellsandextracts.Forsaturationbindinganalysis,bacterialextracts(100μgofprotein)areincubatedat4°Cfor3hinbuffercontaining10mMTris(pH8.0),50mMKCl,10mMdithiothreitolwith[3H]-BRL49653(specificactivity,40Ci/mmol)inthepresenceorabsenceofunlabeledRosiglitazone.Boundisseparatedfromfreeradioactivitybyelutionthrough1-mLSephadexG-25desaltingcolumns.Boundradioactivityelutedinthecolumnvoidvolumeandisquantitatedbyliquidscintillationcounting[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.CellAssay[1]C3H10T1/2cellsaregrownina24-wellplateinDMEmediumsupplementedwith10%fetalcalfserum.Mediumandcompound(Rosiglitazone)areexchangedevery3days.Cellsarestainedatday7withOilRedOandphotographed[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalRatsareintravenouslyinjectedwith38mg/kgstreptozotocinandafter48h,diabetesisidentifiedbyurinaryAdministration[2]glucosuriaandthenrandombloodsugarismeasuredandthisdayisregardedasday0.Animalswithaserumglucoselevelof220-300mg/dLareselectedtobeusedinthisstudy.Ratsarerandomlyseparatedintofivegroupsfordailydrugadministrationfor8weeks:group1:controlnondiabeticratsgivenavehicleonly(0.5mL/kgof0.5%carboxymethylcelleluseorally),group2:controldiabeticratsgivenavehicle,group3:diabeticratsreceivingRosiglitazone(5mg/kgorally),group4:diabeticratsreceivinglosartan(2mg/kg,orally),andgroup5:diabeticratsreceivingbothRosiglitazoneandlosartan[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•CancerCell.2024May13;42(5):869-884.e9.•Circulation.2022Nov30.•CellMetab.2023Dec5;35(12):2165-2182.e7.•CellMetab.2023Sep7;S1550-4131(23)00304-2.•CellMetab.2021Mar2;33(3):581-597.e9.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LehmannJM,etal.Anantidiabeticthiazolidinedioneisahighaffinityligandforperoxisomeproliferator-activatedreceptorgamma(PPAR2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEgamma).JBiolChem.1995Jun2;270(22):12953-6.[2].WillsonTM,etal.Thestructure-activityrelationshipbetweenperoxisomeproliferator-activatedreceptorgammaagonismandtheantihyperglycemicactivityofthiazolidinediones.JMedChem.1996Feb2;39(3):665-8.[3].ThouennonE,etal.Rosiglitazone-activatedPPARγinducesneurotrophicfactor-α1transcriptioncontributingtoneuroprotection.JNeurochem.2015Aug;134(3):463-70.[4].MajeedY,etal.RapidandcontrastingeffectsofrosiglitazoneontransientreceptorpotentialTRPM3andTRPC5channels.MolPharmacol.2011Jun;79(6):1023-30.[5].AteyyaH,etal.Beneficialeffectsofrosiglitazoneandlosartancombinationin