请使用支持JavaScript的浏览器! Medchemexpress/Dapagliflozin(Synonyms: BMS-512148)/HY-10450/100mg_蚂蚁淘,【正品极速】生物医学科研用品轻松购|ebiomall 蚂蚁淘商城
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Medchemexpress/Dapagliflozin(Synonyms: BMS-512148)/HY-10450/100mg
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Medchemexpress/Dapagliflozin(Synonyms: BMS-512148)/HY-10450/100mg
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4000-520-616
Dapagliflozinisanewpharmacologicaltherapyfortype2diabetes,andinhibitssodium/glucosecotransporter2(SGLT2),whichresultsinexcretionofglucoseintotheurine.
Description

Dapagliflozinisanewpharmacologicaltherapyfortype2diabetes,andinhibitssodium/glucosecotransporter2(SGLT2),whichresultsinexcretionofglucoseintotheurine.

InVitro

DapagliflozinpretreatmentofhypoxicHK2cellssignificantlyimprovesthecellviABIlityinadose-dependentmanner.DapagliflozindecreasesBaxexpression,theBax/Bcl2ratio,andPARPexpressioninhypoxicHK2cells[2].

InVivo

At11mMglucose,dapagliflozinraisesglucagonreleasefrom18%to32%ofcontrol,whiletheeffectofdapagliflozinadditionisminorat1mMglucose.Attheintermediateglucoseconcentrationof6mM,glucagonsecretionisestimatedtobe24%and30%ofcontrolintheabsenceorpresenceofdapagliflozin,respectively[1].DapagliflozinpretreatmentsignificantlyreducesthenumberofTUNEL-positivecellsinIR-injuredkidneys.DapagliflozinpretreatmentsignificantlyelevatestheHIF1expressioninIR-injuredrenaltubularcellsfrommice[2].Dapagliflozin(10mg/kg,o.p.)causesamarkedincreaseinurinaryglucoseinSGLT2i-mice.DapagliflozinacutelysuppressesBATThermogenesisbyreducingsympatheticnerveactivity.Dapagliflozinenhanceshepaticgluconeogenesisandglycogenolysis[3].

ClinicalTrial
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References
  • [1].PedersenMG,etal.Dapagliflozinstimulatesglucagonsecretionathighglucose:experimentsandmathematicalsimulationsofhumanA-cells.SciRep.2016Aug18;6:31214.

    [2].Yoon-KyungChang,etal.Dapagliflozin,SGLT2Inhibitor,AttenuatesRenalIschemia-ReperfusionInjury.PLoSOne.2016;11(7):e0158810.

    [3].ChibaY,etal.Dapagliflozin,aSodium-GlucoseCo-Transporter2Inhibitor,AcutelyReducesEnergyExpenditureinBATviaNeuralSignalsinMice.PLoSOne.2016Mar10;11(3):e0150756.

    [4].AkahaneK,etal.EfficacyofMitiglinideCombinedwithDapagliflozininStreptozotocin-nicotinamide-inducedType2DiabeticRatsandinZuckerFattyRats.DrugRes(Stuttg).2015Aug;65(8):416-21.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.4458mL12.2288mL24.4577mL
5mM0.4892mL2.4458mL4.8915mL
10mM0.2446mL1.2229mL2.4458mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[2]

Toperformthecellsurvivalassay,cellsarecollectedafter24hincubationwithvehicleordapagliflozinpretreatmentin30-minischemiaandsurvivingcellsarecountedwithTrypanbluestaining.Thepercentagesurvivalisdeterminedbyquantizationoftherelativeviablenumberoftreatedcellsdividedbytheviablenumberofuntreatedcells.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
[1]

10-week-oldmaleC57BL/6miceweighing30-33geacharedividedintofivegroups:vehicle(Vh)-treatedsham(n=5),dapagliflozin-treatedsham(n=5),Vh-treatedIR(n=7),dapagliflozin-treatedIR(n=7),andalbendazoleanddapagliflozintreatedIR(n=7).Dapagliflozinisadministratedviaoralgavageatadoseof10mg/kg/dayfor2days,starting24hbeforesurgery.Albendazoleisinjectedsubcutaneously1hbeforeIRsurgery.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References
  • [1].PedersenMG,etal.Dapagliflozinstimulatesglucagonsecretionathighglucose:experimentsandmathematicalsimulationsofhumanA-cells.SciRep.2016Aug18;6:31214.

    [2].Yoon-KyungChang,etal.Dapagliflozin,SGLT2Inhibitor,AttenuatesRenalIschemia-ReperfusionInjury.PLoSOne.2016;11(7):e0158810.

    [3].ChibaY,etal.Dapagliflozin,aSodium-GlucoseCo-Transporter2Inhibitor,AcutelyReducesEnergyExpenditureinBATviaNeuralSignalsinMice.PLoSOne.2016Mar10;11(3):e0150756.

    [4].AkahaneK,etal.EfficacyofMitiglinideCombinedwithDapagliflozininStreptozotocin-nicotinamide-inducedType2DiabeticRatsandinZuckerFattyRats.DrugRes(Stuttg).2015Aug;65(8):416-21.

MolecularWeight

408.87

Formula

C₂₁H₂₅ClO₆

CASNo.

461432-26-8

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

Dapagliflozinispreparedin0.5%CMC+distilledwater(DW)[4].

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

References
  • [1].PedersenMG,etal.Dapagliflozinstimulatesglucagonsecretionathighglucose:experimentsandmathematicalsimulationsofhumanA-cells.SciRep.2016Aug18;6:31214.

    [2].Yoon-KyungChang,etal.Dapagliflozin,SGLT2Inhibitor,AttenuatesRenalIschemia-ReperfusionInjury.PLoSOne.2016;11(7):e0158810.

    [3].ChibaY,etal.Dapagliflozin,aSodium-GlucoseCo-Transporter2Inhibitor,AcutelyReducesEnergyExpenditureinBATviaNeuralSignalsinMice.PLoSOne.2016Mar10;11(3):e0150756.

    [4].AkahaneK,etal.EfficacyofMitiglinideCombinedwithDapagliflozininStreptozotocin-nicotinamide-inducedType2DiabeticRatsandinZuckerFattyRats.DrugRes(Stuttg).2015Aug;65(8):416-21.

Purity:99.89%