E-Z-GSK5182-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemE(E/Z)-GSK5182Cat.No.:HY-111226A分⼦式:C₂₇H₃₁NO₃分⼦量:417.54作⽤靶点:EstrogenReceptor/ERR;ReactiveOxygenSpecies作⽤通路:Others;Immunology/Inflammation;MetabolicEnzyme/Protease;NF-κB储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥75mg/mL(179.62mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3950mL11.9749mL23.9498mL5mM0.4790mL2.3950mL4.7900mL10mM0.2395mL1.1975mL2.3950mL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.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥3.75mg/mL(8.98mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:3.75mg/mL(8.98mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥3.75mg/mL(8.98mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性(E/Z)-GSK5182(E)-GSK5182和(Z)-GSK5182的消旋体。GSK5182⼀种⾼效选择性，具有⼝服活性的ERRγ反向激动剂，其IC50值为79nM。GSK5182还能增加肝癌细胞中reactiveoxyenspecies(ROS)的产⽣。REFERENCES[1].KimJH,etal.Estrogen-relatedreceptorγisupregulatedinlivercanceranditsinhibitionsuppresseslivercancercellproliferationviainductionofp21andp27.ExpMolMed.2016Mar4;48:e213.[2].MisraJ,etal.ERRγ:aJuniorOrphanwithaSeniorRoleinMetabolism.TrendsEndocrinolMetab.2017Apr;28(4):261-272.[3].KimDK,etal.InverseagonistofnuclearreceptorERRγmediatesantidiabeticeffectthroughinhibitionofhepaticgluconeogenesis.Diabetes.2013Sep;62(9):3093-102.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400