Dapagliflozin-BMS-512148-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEDapagliflozinCat.No.:HY-10450CASNo.:461432-26-8Synonyms:BMS-512148分?式:C??H??ClO?分?量:408.87作?靶點(diǎn):SGLT作?通路:MembraneTransporter/IonChannel儲(chǔ)存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥100mg/mL(244.58mM)H2O:50mg/mL(122.29mM;Needultrasonic)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.4458mL12.2288mL24.4577mL5mM0.4892mL2.4458mL4.8915mL10mM0.2446mL1.2229mL2.4458mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請(qǐng)依序添加每種溶劑：1%DMSO>>99%salineSolubility:≥0.5mg/mL(1.22mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.09mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.09mM);Clearsolution4.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.09mM);Clearsolution5.請(qǐng)依序添加每種溶劑：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(6.11mM);Clearsolution6.請(qǐng)依序添加每種溶劑：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.11mM);Clearsolution7.請(qǐng)依序添加每種溶劑：PBSSolubility:33.33mg/mL(81.52mM);Clearsolution;Needultrasonicandwarmingandheatto60°CBIOLOGICALACTIVITY?物活性Dapagliflozin(BMS-512148)?種競(jìng)爭(zhēng)性葡萄糖協(xié)同轉(zhuǎn)運(yùn)蛋?2(SGLT2)抑制劑，可導(dǎo)致尿液中葡萄糖的排泄，?于糖尿病(DM)的研究。Dapagliflozin誘導(dǎo)HIF1表達(dá)并減輕腎臟IR損傷。IC50&TargetSGLT2[1]體外研究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?邊的抑制劑?師www.MedChemE體內(nèi)研究Dapagliflozin(oraladministration;10mg/kg)causesamarkedincreaseinurinaryglucoseinSGLT2i-mice,suppressesBATthermogenesisbyreducingsympatheticnerveactivityandenhanceshepaticgluconeogenesisandglycogenolysis[3].戶(hù)使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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