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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/Dapagliflozin（同义词：BMS-512148）/HY-10450/5mg
商品详细Medchemexpress/Dapagliflozin（同义词：BMS-512148）/HY-10450/5mg
Medchemexpress/Dapagliflozin（同义词：BMS-512148）/HY-10450/5mg
Medchemexpress/Dapagliflozin（同义词：BMS-512148）/HY-10450/5mg
商品编号： HY-10450-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥1100.00
美元价： 660.00
产地： 美国(厂家直采)
公司：
产品分类： 小分子
公司分类： Small_molecule
联系Q Q： 3392242852
电话号码： 4000-520-616
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商品介绍
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%