Dapagliflozin-BMS-512148-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEDapagliflozinCat.No.:HY-10450CASNo.:461432-26-8Synonyms:BMS-512148分⼦式:C₂₁H₂₅ClO₆分⼦量:408.87作⽤靶点:SGLT作⽤通路:MembraneTransporter/IonChannel储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:≥100mg/mL(244.58mM)H2O:50mg/mL(122.29mM;Needultrasonic)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4458mL12.2288mL24.4577mL5mM0.4892mL2.4458mL4.8915mL10mM0.2446mL1.2229mL2.4458mL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(sealedstorage,awayfrommoisture)。-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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：1%DMSO>>99%salineSolubility:≥0.5mg/mL(1.22mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.09mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.09mM);Clearsolution4.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.09mM);Clearsolution5.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(6.11mM);Clearsolution6.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.11mM);Clearsolution7.请依序添加每种溶剂：PBSSolubility:33.33mg/mL(81.52mM);Clearsolution;Needultrasonicandwarmingandheatto60°CBIOLOGICALACTIVITY⽣物活性Dapagliflozin(BMS-512148)⼀种竞争性葡萄糖协同转运蛋⽩2(SGLT2)抑制剂，可导致尿液中葡萄糖的排泄，⽤于糖尿病(DM)的研究。Dapagliflozin诱导HIF1表达并减轻肾脏IR损伤。IC50&TargetSGLT2[1]体外研究Dapagliflozin(0-10μM；24hours)significantlyincreasesthecellsurvivalinhypoxicHK2cellinadose-dependentmanner[2].Dapagliflozin(0-10μM；2hours)increasestheHIF1expression,increasesAMPKandEKRphosphorylationinhypoxicHK2cells,butshowsnoeffectonthephosphorylationofAMPKandERKinnormoxicHK2cells[2]..CellViabilityAssay[1]CellLine:HypoxicHK2cellsConcentration:0μM,1μM,2μM,5μM,10μMIncubationTime:24hoursResult:Improvedthecellviabilityinadose-dependentmannercomparedwithcontrolcells.WesternBlotAnalysis[1]CellLine:HypoxicHK2cells,NormoxicHK2cellsConcentration:0μM,1μM,2μM,5μM,10μMIncubationTime:24hoursResult:InducedHIF1expressioninhypoxicandnormoxicHK2cells.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体内研究Dapagliflozin(oraladministration;10mg/kg)causesamarkedincreaseinurinaryglucoseinSGLT2i-mice,suppressesBATthermogenesisbyreducingsympatheticnerveactivityandenhanceshepaticgluconeogenesisandglycogenolysis[3].户使⽤本产品发表的科研⽂献•CardiovascRes.02November2020.•EBioMedicine.2022,86:104342.•MolMetab.2019Jan;19:1-12.•OxidMedCellLongev.2022Jan28;2022:8502059.•ActaPharmacolSin.2021Dec1.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].PedersenMG,etal.Dapagliflozinstimulatesglucagonsecretionathighglucose:experimentsandmathematicalsimulationsofhumanA-cells.SciRep.2016Aug18;6:31214.[2].ChibaY,etal.Dapagliflozin,aSodium-GlucoseCo-Transporter2Inhibitor,AcutelyReducesEnergyExpenditureinBATviaNeuralSignalsinMice.PLoSOne.2016Mar10;11(3):e0150756.[3].ChangYK,etal.Dapagliflozin,SGLT2Inhibitor,AttenuatesRenalIschemia-ReperfusionInjury.PLoSOne.2016Jul8;11(7):e0158810.McePdfHeightCaution:Pr