Pioglitazone-U-72107-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPioglitazoneCat.No.:HY-13956CASNo.:111025-46-8Synonyms:U72107分⼦式:C₁₉H₂₀N₂O₃S分⼦量:356.44作⽤靶点:PPAR;Ferroptosis作⽤通路:CellCycle/DNADamage;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:40mg/mL(112.22mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8055mL14.0276mL28.0552mL5mM0.5611mL2.8055mL5.6110mL10mM0.2806mL1.4028mL2.8055mL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：0.5%CMC-Na/salinewater1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:10mg/mL(28.06mM);Suspenedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:2.08mg/mL(5.84mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.84mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Pioglitazone(U72107)⼀种具有⼝服活性的选择性PPARγ(peroxisomeproliferator-activatedreceptor)激动剂，⾼亲和⼒结合到PPARγ配体结合域，作⽤于⼈和⿏PPARγ的EC50分别为0.93和0.99μM。Pioglitazone可⽤于糖尿病研究。IC50&TargethPPARγmousePPARγhPPARδhPPARα0.93μM(EC50)0.99μM(EC50)43μM(EC50)100μM(EC50)mousePPARα100μM(EC50)体外研究Pioglitazone(0.5or1μM,5days)cancompletelypreventAGEs(advancedglycationend-products)-inducedβ-cellnecrosisandtheincreaseofcaspase-3therebyavoidingtheimpairedviabilitycausedbyAGEsinpancreaticbetacelllineHIT-T15[2].Pioglitazone(1μM,1h)canstimulateinsulinsecretioninducedbylowglucoseconcentrationandattenuatetheGSSG/GSHratioincellsculturedwithAGEs[2].体内研究Pioglitazone(oralgavage,10or30mg/kg,oncedaily,14days)caninduceimprovementsininsulinresistanceanddiabetesthatmaybelipocalin-dependentintheliverbutnotinskeletalmuscle[3].Pioglitazone(oralgavage,10mg/kg,oncedaily,4weeks)cansignificantlyreducebodyweight(BW),cardiachypertrophy,elevatedbloodglucoselevelsandimprovetheassociateddyslipidemia[4].AnimalModel:ob/obandadipo-/-ob/obmicewithaC57Bl/6background[3]Dosage:10or30mg/kgAdministration:Oralgavage;oncedaily;14daysResult:Showednochangesofserum-freefattyacidandtriglyceridelevelsaswellasadipocytesizesinob/obandadipo-/-ob/obC57BL/6miceat10mg/kgbutsignificantlyreducedtoasimilardegreeat30mg/kg.AlsoshowednochangesofexpressionsofTNFαandresistininadiposetissuesofob/obandadipo-/-ob/obmiceat10mg/kgbutdecreasedat30mg/kg.AnimalModel:MaleWistaralbinorats[4]Dosage:10mg/kg2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAdministration:Oralgavage;oncedaily;4weeksResult:Decreasedtheelevatedserumlevelsofbothcreatinineandcreatinekinase-MB(CK-MB),TGF-β1geneexpressionandregulatedtheexpressionofMMP-2/TIMP-2system.户使⽤本产品发表的科研⽂献•CellMetab.2021Mar2;33(3):581-597.e9.•CellStemCell.2022Sep1;29(9):1366-1381.e9.•CancerRes.2022Apr15;82(8):1503-1517.•BrJPharmacol.2021Jun;178(11):2305-2323.•GutMicrobes.2022,14(1):2139978.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].KuwabaraK,etal.Anovelselectiveperoxisomeproliferator-activatedreceptoralphaagonist,2-methyl-c-5-[4-[5-methyl-2-(4-methylphenyl)-4-oxazolyl]butyl]-1,3-dioxane-r-2-carboxylicacid(NS-220),potentlydecreasesplasmatriglycerideandglucoseleve[2].PudduA,etal.Pioglitazoneattenuatesthedetrimentaleffectsofadvancedglycationend-productsinthepancreaticbetacelllineHIT-T15.RegulPept.2012Aug20;177(1-3):79-84.[3].KubotaN,etal.Pioglitazoneamelioratesinsulinresistanceanddiabetesbybothadiponectin-dependentand-independentpathways.JBiolChem.2006Mar31;281(13):8748-55.[4].ElrashidyRA,etal.Pioglitazoneattenuatescardiacfibrosisandhypertrophyinaratmodelofdiabeticnephropathy.JCardiovascPharmacolTher.2012Sep;17(3):324