Ertugliflozin-L-pyroglutamic-acid-PF-04971729-L-pyroglutamic-acid-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEErtugliflozinL-pyroglutamicacidCat.No.:HY-15461ACASNo.:1210344-83-4Synonyms:PF-04971729L-pyroglutamicacid分⼦式:C₂₇H₃₂ClNO₁₀分⼦量:566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:≥125mg/mL(220.85mM)H2O:5mg/mL(8.83mM;ultrasonicandwarmingandheatto60°C)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7668mL8.8339mL17.6678mL5mM0.3534mL1.7668mL3.5336mL10mM0.1767mL0.8834mL1.7668mL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1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(3.67mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.67mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.67mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性ErtugliflozinL-pyroglutamicacid(PF-04971729L-pyroglutamicacid)有效的、选择性的、具有⼝服活性的钠离⼦依赖的葡萄糖协同转运蛋⽩2(SGLT2)的有效选择性抑制剂。ErtugliflozinL-pyroglutamicacid对h-SGLT2的IC50值为0.877nM[1][2]。ErtugliflozinL-pyroglutamicacid可⽤于2型糖尿病的研究[3]。IC50&TargetIC50:0.877nM(h-SGLT2)[1].体外研究ErtugliflozinL-pyroglutamicacid(PF-04971729L-pyroglutamicacid)demonstrates>2000-foldselectivityforSGLT2inhibition(relativetoSGLT1)invitro[3].体内研究ErtugliflozinL-pyroglutamicacid(PF-04971729L-pyroglutamicacid)revealsaconcentration-dependentglucosuriaafteroraladministrationtorats[3].户使⽤本产品发表的科研⽂献•BiochemPharmacol.2016Feb1;101:27-39.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MascittiV,etal.Discoveryofaclinicalcandidatefromthestructurallyuniquedioxa-bicyclo[3.2.1]octaneclassofsodium-dependentglucosecotransporter2inhibitors.JMedChem.2011Apr28;54(8):2952-60.[2].MiaoZ,etal.Pharmacokinetics,metabolism,andexcretionoftheantidiabeticagentertugliflozin(PF-04971729)inhealthymalesubjects.DrugMetabDispos.2013Feb;41(2):445-56.[3].KalgutkarAS,etal.PreclinicalspeciesandhumandispositionofPF-04971729,aselectiveinhibitorofthesodium-dependentglucosecotransporter2andclinicalcandidateforthetreatmentoftype2diabetesmellitus.DrugMetabDispos.2011Sep;39(9):16McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalappl