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

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemERosiglitazoneCat.No.:HY-17386CASNo.:122320-73-4Synonyms:BRL49653分⼦式:C₁₈H₁₉N₃O₃S分⼦量:357.43作⽤靶点:PPAR;TRPChannel;Autophagy;Ferroptosis;Apoptosis作⽤通路:CellCycle/DNADamage;MembraneTransporter/IonChannel;NeuronalSignaling;Autophagy;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(699.44mM;Needultrasonic)Ethanol:2mg/mL(5.60mM;ultrasonicandwarmingandheatto60°C)H2O:<0.1mg/mL(ultrasonic)(insoluble)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7978mL13.9888mL27.9775mL5mM0.5596mL2.7978mL5.5955mL10mM0.2798mL1.3989mL2.7978mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现1/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.82mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.82mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:2.5mg/mL(6.99mM);Suspendedsolution;Needultrasonic4.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(6.99mM);Clearsolution5.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.99mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Rosiglitazone(BRL49653)⼀种具有⼝服活性的PPARγ选择性激动剂(EC50:60nM,Kd:40nM)。Rosiglitazone⼀种TRPC5激活剂(EC50:30μM)和TRPM3抑制剂。Rosiglitazone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Rosiglitazone(0.1-10μM,72h)resultsinpluripotentC3H10T1/2stemcelldifferentiationtoadipocytes[1].Rosiglitazone(1μM,24h)activatesPPARγ,whichbindstoNF-α1promotertoactivategenetranscriptioninneurons[3].Rosiglitazone(1μM,24h)protectsNeuro2Acellsandhippocampalneuronsagainstoxidativestress,and

up-regulatesBCL-2expressioninanNF-α1-dependentmanner[3].Rosiglitazone(0.01-100μM,15min)inhibitsTRPM3withIC50valuesof9.5and4.6μMagainstnifedipine-

andPregS-evokedactivityrespectively[4].Rosiglitazone(0.5-50μM,7days)inhibitsovariancancercellproliferation[7].Rosiglitazone(5μM,7days)suppressesOlaparib(HY-10162)‑inducedalterationsofcellularsenescenceandpromotesapoptosisinA2780andSKOV3cells[7].CellProliferationAssay[7]CellLine:A2780andSKOV3cellsConcentration:0.5-50μMIncubationTime:1-7daysResult:Inhibitedcellproliferationinatime‑dependentandconcentration‑dependentmanner.WesternBlotAnalysis[3]2/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellLine:HippocampalneuronsConcentration:1μMIncubationTime:24hResult:IncreasedNF-α1andBCL-2proteinlevel.体内研究Rosiglitazone(oraladministration,5mg/kg,dailyfor8weeks)decreasestheserumglucoseindiabeticrats[5].Rosiglitazone(intraperitonealinjection,3mg/kg/day)amelioratesairwayinflammationinducedbycigarettesmokeviainhibitingtheM1macrophagepolarizationbyactivatingPPARγandRXRαinmaleWistarrats[6].Rosiglitazone(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.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.MedChemE3/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.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-α1tra