Empagliflozin-BI-10773-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEmpagliflozinCat.No.:HY-15409CASNo.:864070-44-0Synonyms:BI10773分⼦式:C₂₃H₂₇ClO₇分⼦量:450.91作⽤靶点:SGLT作⽤通路:MembraneTransporter/IonChannel储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(110.89mM;Needultrasonic)H2O:0.11mg/mL(0.24mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2177mL11.0887mL22.1774mL5mM0.4435mL2.2177mL4.4355mL10mM0.2218mL1.1089mL2.2177mL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。-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：0.5%HPMCSolubility:5mg/mL(11.09mM);Suspensionsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.61mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.61mM);Clearsolution4.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.61mM);Clearsolution5.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.87mg/mL(6.36mM);Clearsolution6.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.87mg/mL(6.36mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Empagliflozin(BI10773)⼀种选择性钠葡萄糖协同转运蛋⽩-2(SGLT-2)抑制剂，抑制⼈SGLT-2的IC50为3.1nM[1]。IC50&TargetIC50:3.1nM(SGLT-2),1.1μM(SGLT-5),2μM(SGLT-6),8.3μM(SGLT-1),11μM(SGLT-4)[1]体外研究EmpagliflozinisapotentandcompetitiveSGLT-2inhibitorwithanexcellentselectivityprofileandthehighestselectivitywindowofthetestedSGLT-2inhibitorsoverhSGLT-1.Empagliflozininhibitstheuptakeof[14C]-alpha-methylglucopyranoside(AMG)viahSGLT-2inadose-dependentmannerwithanIC50of3.1nM,butislesspotentforotherSGLTs(IC50range:1100-11000nM).[3H]-EmpagliflozindisplaysahighaffinityforSGLT-2withameanKdof57±37nMintheabsenceofglucoseinkineticbindingexperiments[1].体内研究Glucoseintoleranceissignificantlyimprovedafter8daysofEmpagliflozintreatmentateitherdose(3mg/kgEmpagliflozin3058±180vs10mg/kgEmpagliflozin3090±219).Therefore,acutetreatmentwithEmpagliflozinhasabeneficialeffectonhyperglycemiaandglucoseintolerance.SincetherearenosignificantdifferencesinbloodglucosehomeostasiswiththetwodifferentdosesofEmpagliflozin,andrandombloodglucoselevelsofT1DMmicearesignificantlyimprovedby3mg/kgofEmpagliflozin,theeffectofthelowerdoseofEmpagliflozin(3mg/kg)isinvestigatedonpreservingβ-cellmassandfunction[2].PROTOCOLAnimalMice[2]Administration[2]MaleC57BL/6Jmice(10weeksofage)areused.Empagliflozinisdissolvedinhydroxyethylcellulose(HEC)andadministeredtomiceintheexperimentalgroup(3or10mg/kg)byoralgavageoncedailyfor8days,whereasthevehiclegroupisgivensamevolumeofHECalone.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE户使⽤本产品发表的科研⽂献•ProteinCell.2022May;13(5):336-359.•BasicResCardiol.2022Sep28;117(1):47.•ActaBiomater.2022Feb18;S1742-7061(22)00096-4.•Diabetologia.2017Mar;60(3):568-573.•JACCBasicTranslSci.2019Sep4;4(5):575-591.Seemorecustomervalidationsonwww.MedChemEREFERENCES[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.[4].SakaedaT,etal.Susceptibilitytoseriousskinandsubcutaneoustissuedisordersandskintissuedistributionofsodium-dependentglucoseco-transportertype2(SGLT2)inhibitors.IntJMedSci.2018Jun13;