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Medchemexpress/Empagliflozin(Synonyms: BI 10773)/HY-15409/100mg

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Medchemexpress/Empagliflozin(Synonyms: BI 10773)/HY-15409/100mg

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MedChemExp

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HY-15409-10mM*1mLinDMSO

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4000-520-616

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Empagliflozinisaselectivesodiumglucosecotransporter-2(SGLT-2)inhibitorwithanIC₅₀of3.1nMforhSGLT-2.

CustomerValidation

•Diabetologia.2017Mar;60(3):568-573.
•JChromatogrBAnalytTechnolBiomedLifeSci.2016Aug1;1027:227-33.
•JChromatogrBAnalytTechnolBiomedLifeSci.2015Jul14;1000:22-28.
•BiomedChromatogr.2016Oct;30(10):1549-55.
•JACCBasicTranslSci.2017Aug;2(3):347-354.

Description	Empagliflozinisaselectivesodiumglucosecotransporter-2(SGLT-2)inhibitorwithanIC₅₀of3.1nMforhSGLT-2.
IC₅₀&Target	IC50:3.1nM(SGLT-2),1.1μM(SGLT-5),2μM(SGLT-6),8.3μM(SGLT-1),11μM(SGLT-4)^[1]
InVitro	EmpagliflozinisapotentandcompetitiveSGLT-2inhibitorwithanexcellentselectivityprofileandthehighestselectivitywindowofthetestedSGLT-2inhibitorsoverhSGLT-1.Empagliflozininhibitstheuptakeof[¹⁴C]-alpha-methylglucopyranoside(AMG)viahSGLT-2inadose-dependentmannerwithanIC₅₀of3.1nM,butislesspotentforotherSGLTs(IC₅₀range:1100-11000nM).[³H]-EmpagliflozindisplaysahighaffinityforSGLT-2withameanK_dof57±37nMintheabsenceofglucoseinkineticbindingexperiments^[1].
InVivo	Glucoseintoleranceissignificantlyimprovedafter8daysofEmpagliflozintreatmentateitherdose(3mg/kgEmpagliflozin3058±180vs10mg/kgEmpagliflozin3090±219).Therefore,acutetreatmentwithEmpagliflozinhasabeneficialeffectonhyperglycemiaandglucoseintolerance.SincetherearenosignificantdifferencesinbloodglucosehomeostasiswiththetwodifferentdosesofEmpagliflozin,andrandombloodglucoselevelsofT1DMmicearesignificantlyimprovedby3mg/kgofEmpagliflozin,theeffectofthelowerdoseofEmpagliflozin(3mg/kg)isinvestigatedonpreservingβ-cellmassandfunction^[2].
References	[1].GremplerR,etal.Empagliflozin,anovelselectivesodiumglucosecotransporter-2(SGLT-2)inhibitor:characterisationandcomparisonwithotherSGLT-2inhibitors.DiabetesObesMetab.2012Jan;14(1):83-90. [2].ChengST,etal.TheEffectsofEmpagliflozin,anSGLT2Inhibitor,onPancreaticβ-CellMassandGlucoseHomeostasisinType1Diabetes.PLoSOne.2016Jan25;11(1):e0147391. [3].NikoleJ.ByrNEBSc,etal.EmpagliflozinPreventsWorseningofCardiacFunctioninanExperimentalModelofPressureOverload-InducedHeartFailure.JACCBasicTranslSci.2017Aug;2(4):347-354.

PreparingStockSolutions

ConcentrationVolumeMass	1mg	5mg	10mg

1mM	2.2177mL	11.0887mL	22.1774mL
5mM	0.4435mL	2.2177mL	4.4355mL
10mM	0.2218mL	1.1089mL	2.2177mL

Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.

KinaseAssay
^[1]

Membranes(60μg/well)areassayedina10mM4-(2-hydroxyethyl)-1-piperazineethanesulfonicacid(HEPES)buffer(pH7.4)containing137mMNaClinthepresenceorabsenceof20mMglucoseandindicatedconcentrationsof[³H]-Empagliflozinin96-wellplatesatroomtemperaturefor2h.IncubationsarestoppedbyrapidfiltrationthroughGF/BFilterplatesimpregnatedwithpolyethyleneimine0.5%andprewettedwith0.9%NaClsolution,andwashedfourtimeswith0.9%NaClsolution(4°C)usingaHarvesterFiltermate96.Filterplatesaredriedfor2hand50μLofMicroscint20isaddedtoeachwell.RADIoactivityretainedonthefiltersismeasuredusingtheTopCountNXT.Inparallel,theactualamountofactivityusedintheassaysisdeterminedbyaddingthesameamountof[³H]-Empagliflozinthatisaddedperwellintheradioligandbindingstudiesand4mLUltimaGoldScintilatorinto5mLvialsandmeasuringusingaTricarb2900TR.Non-specific[³H]-Empagliflozin-bindingisdeterminedinthepresenceof30μMdapagliflozin^[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
^[2]

Empagliflozinisdissolvedinhydroxyethylcellulose(HEC)(Mice)^[2].

Mice^[2]
MaleC57BL/6Jmice(10weeksofage)areused.Empagliflozinisdissolvedinhydroxyethylcellulose(HEC)andadministeredtomiceintheexperimentalgroup(3or10mg/kg)byoralgavageoncedailyfor8days,whereasthevehiclegroupisgivensamevolumeofHECalone.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

[1].GremplerR,etal.Empagliflozin,anovelselectivesodiumglucosecotransporter-2(SGLT-2)inhibitor:characterisationandcomparisonwithotherSGLT-2inhibitors.DiabetesObesMetab.2012Jan;14(1):83-90.
[2].ChengST,etal.TheEffectsofEmpagliflozin,anSGLT2Inhibitor,onPancreaticβ-CellMassandGlucoseHomeostasisinType1Diabetes.PLoSOne.2016Jan25;11(1):e0147391.
[3].NikoleJ.ByrneBSc,etal.EmpagliflozinPreventsWorseningofCardiacFunctioninanExperimentalModelofPressureOverload-InducedHeartFailure.JACCBasicTranslSci.2017Aug;2(4):347-354.

MolecularWeight

450.91

Formula

C₂₃H₂₇ClO₇

CASNo.

864070-44-0

Storage

Powder	-20°C	3years
	4°C	2years
Insolvent	-80°C	6months
	-20°C	1month

Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

Empagliflozinisprepparedin0.5%hydroxyethylcellulose^[3].

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

References

[1].GremplerR,etal.Empagliflozin,anovelselectivesodiumglucosecotransporter-2(SGLT-2)inhibitor:characterisationandcomparisonwithotherSGLT-2inhibitors.DiabetesObesMetab.2012Jan;14(1):83-90.
[2].ChengST,etal.TheEffectsofEmpagliflozin,anSGLT2Inhibitor,onPancreaticβ-CellMassandGlucoseHomeostasisinType1Diabetes.PLoSOne.2016Jan25;11(1):e0147391.
[3].NikoleJ.ByrneBSc,etal.EmpagliflozinPreventsWorseningofCardiacFunctioninanExperimentalModelofPressureOverload-InducedHeartFailure.JACCBasicTranslSci.2017Aug;2(4):347-354.

Purity:99.91%ee.:98.83%

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