ELOVL6-IN-3-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEELOVL6-IN-3Cat.No.:HY-139451CASNo.:712346-06-0分?式:C??H??F?N?O?分?量:495.49作?靶點(diǎn):Others作?通路:Others儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性ELOVL6-IN-1?種有效的，具有?服活性和選擇性ELOVL6抑制劑。ELOVL6-IN-1對(duì)??ELOVL6的抑制作?呈劑量依賴性，IC50值為0.350μM。ELOVL6-IN-1對(duì)丙?酰輔酶a(Ki=994nM)和對(duì)棕櫚酰輔酶a具有?競(jìng)爭(zhēng)性抑制ELOVL6作?[1]。IC50&TargetIC50:0.35μM(ELOVL6),Ki:994nM(ELOVL6)[1]體外研究ELOVL6-IN-1hassufficientlylipophilichavingthepotentialtopenetratetheintracellularspaceinapassivediffusionmanner[1].體內(nèi)研究ELOVL6-IN-1(10mg/kg;p.o.;0~2hours)displaysappreciableplasmaandliverexposure[1].?ELOVL6-IN-1(10and30mg/kg;p.o.;0~2hours)reducestheelongationindexoftheliverlipids[1].?ELOVL6-IN-1(100mg/kg;p.o.;2days)reducestheelongationindexofthetotalfattyacidsoftheliver[1].REFERENCES[1].TakahashiT,NagaseT,SasakiT,etal.Synthesisandevaluationofanovelindoledioneclassoflongchainfattyacidelongase6(ELOVL6)inhibitors.JMedChem.2009;52(10):3142-3145.[2].ZhengJunxia,WuZhiwei,DaiMibei,XuZhihui,LiXiaomei,ZhuShanshan,LinChuyun,HuPeijian,ZhangLuo,HuangHuarong,ZhaoSuqing,ZhangKunandSunPinghua,QuantitativeStructureActivityRelationshipStudiesonaNovelIndoledionesasLongChainFattyAcidElongase6(ELOVL6)Inhibitors,LettersinDrugDesign&Discovery2011;8(5).[3].ShimamuraK,etal.5,5-Dimethyl-3-(5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)-1-phenyl-3-(trifluoromethyl)-3,5,6,7-tetrahydro-1H-indole-2,4-dione,apotentinhibitorformammalianelongaseoflong-chainfattyacidsfamily6:examinationofitspotentialutilityasapharmacologicaltool.JPharmacolExpTher.2009;330(1):249-256.1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-8