Rosiglitazone-hydrochloride-BRL-49653-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemERosiglitazonehydrochlorideCat.No.:HY-17386ACASNo.:302543-62-0Synonyms:BRL49653hydrochloride分⼦式:C₁₈H₂₀ClN₃O₃S分⼦量:393.89作⽤靶点:PPAR;TRPChannel;Autophagy;Ferroptosis;Apoptosis作⽤通路:CellCycle/DNADamage;MembraneTransporter/IonChannel;NeuronalSignaling;Autophagy;Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Rosiglitazone(BRL49653)hydrochloride⼀种具有⼝服活性的PPARγ选择性激动剂(EC50:60nM,Kd:40nM)。Rosiglitazonehydrochloride⼀种TRPC5激活剂(EC50:30μM)和TRPM3抑制剂。Rosiglitazonehydrochloride可⽤于肥胖、糖尿病、衰⽼、巢癌的研究。IC50&TargetPPARγPPARγTRPC5TRPM340nM(Kd)60nM(EC50)30μM(EC50)体外研究Rosiglitazonehydrochloride(0.1-10μM,72h)resultsinpluripotentC3H10T1/2stemcelldifferentiationtoadipocytes[1].Rosiglitazonehydrochloride(1μM,24h)activatesPPARγ,whichbindstoNF-α1promotertoactivategene

transcriptioninneurons[3].Rosiglitazonehydrochloride(1μM,24h)protectsNeuro2Acellsandhippocampalneuronsagainstoxidative

stress,andup-regulatesBCL-2expressioninanNF-α1-dependentmanner[3].Rosiglitazonehydrochloride(0.01-100μM,15min)inhibitsTRPM3withIC50valuesof9.5and4.6μM

againstnifedipine-andPregS-evokedactivityrespectively[4].Rosiglitazonehydrochloride(0.5-50μM,7days)inhibitsovariancancercellproliferation[7].Rosiglitazonehydrochloride(5μM,7days)suppressesOlaparib(HY-10162)‑inducedalterationsofcellularsenescenceandpromotesapoptosisinA2780andSKOV3cells[7].CellProliferationAssay[7]1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellLine:A2780andSKOV3cellsConcentration:0.5-50μMIncubationTime:1-7daysResult:Inhibitedcellproliferationinatime‑dependentandconcentration‑dependentmanner.WesternBlotAnalysis[3]CellLine:HippocampalneuronsConcentration:1μMIncubationTime:1μMResult:IncreasedNF-α1andBCL-2proteinlevel.体内研究Rosiglitazonehydrochloride(oraladministration,5mg/kg,dailyfor8weeks)decreasestheserumglucoseindiabeticrats[5].Rosiglitazonehydrochloride(intraperitonealinjection,3mg/kg/day)amelioratesairwayinflammationinducedbycigarettesmokeviainhibitingtheM1macrophagepolarizationbyactivatingPPARγandRXRαinmaleWistarrats[6].Rosiglitazonehydrochloride(intraperitonealinjection,10mg/kg,onceevery2days)inhibitssubcutaneousovariancancergrowthinA2780andSKOV3mousesubcutaneousxenograftmodels[7].AnimalModel:Streptozotocin(STZ)-induceddiabeticrats[5]Dosage:5mg/kgAdministration:Oraladministration,dailyfor8weeks.Result:DecreasedIL-6,TNF-α,andVCAM-1levelsindiabeticgroup.DisplayedlowerlevelsoflipidperoxidationandNOxwithanincreaseinaorticGSHandSODlevelscomparedtodiabeticgroups.AnimalModel:MaleWistarrats[6]Dosage:3mg/kg/dayAdministration:Intraperitonealinjection,twiceaday,6daysperweekfor12consecutiveweeksResult:Amelioratedemphysema,elevatedPEF,andhigherleveloftotalcells,neutrophilsandcytokines(TNF-αandIL-1β)inducedbycigarettesmoke(CS).InhibitedCS-inducedM1macrophagepolarizationanddecreasedtheratioofM1/M2.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE户使⽤本产品发表的科研⽂献•Circulation.2022Nov30.•CellMetab.2021Mar2;33(3):581-597.e9.•JExpMed.2022May2;219(5):e20211906.•CancerRes.2022Apr15;82(8):1503-1517.•CellDeathDiffer.2022Nov3.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].HaoshenFeng,etal.RosiglitazoneamelioratedairwayinflammationinducedbycigarettesmokeviainhibitingtheM1macrophagepolarizationbyactivatingPPARγandRXRα.IntImmunopharmacol.2021Aug;97:107809.[2].ZehuaWang,etal.Rosiglitazoneamelioratessenescenceandpromotesapoptosisinovariancancerinducedbyolaparib.CancerChemotherPharmacol.2020Feb;85(2):273-284.[3].LehmannJM,etal.Anantidiabeticthiazolidinedioneisahighaffinityligandforperoxisomeproliferator-activatedreceptorgamma(PPARgamma).JBiolChem.1995Jun2;270(22):12953-6.[4].WillsonTM,etal.Thestructure-activityrelationshipbetweenperoxisomeproliferator-activatedreceptorgammaagonismandtheantihyperglycemicactivityofthiazolidinediones.JMedChem.1996Feb2;39(3):665-8.[5].ThouennonE,etal.Rosiglitazone-activatedPPARγinducesneurotrophicfactor-α1transcriptioncontributingtoneuroprotection.JNeurochem.2015Aug;134(3):463-70.[6].MajeedY,etal.RapidandcontrastingeffectsofrosiglitazoneontransientreceptorpotentialTRPM3andTRPC5channels.MolPharmacol.2011Jun;79(6):1023-30.[7].AteyyaH,etal.Beneficialeffectsofrosiglitazoneandlosartancombinationindiabeticrats.CanJPhysiol