TLX-agonist-3-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETLXagonist3Cat.No.:HY-180403CASNo.:3032232-47-3分⼦式:C₂₅H₂₃F₃N₄O₂分⼦量:468.48作⽤靶点:OrphanNuclearReceptor作⽤通路:VitaminDRelated/NuclearReceptor储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性TLXagonist3⼀种强效且选择性的⽆尾同物(TLX，NR2E1)激动剂，其EC50为0.25μM，Kd为1.6μM。TLXagonist3对相关核受体表现出⾼选择性，并促进TLX寡聚化(EC50=5.0μM)。TLXagonist3可⽤于神经退⾏性疾病的研究[1]。IC50&TargetTLXTLX0.25μM(EC50)1.6μM(Kd)体外研究TLXagonist3(compound10)(2.5-20μM;22h)enhancesTLXoligomerizationinaconcentration-dependentmannerinhomogeneoustime-resolvedfluorescenceresonanceenergytransfer\n(HTRF)-basedassay[1].TLXagonist3activatesfull-lengthhumanTLXinHEK293cellswithanEC50of0.7μM[1].TLXagonist3(3µM;8h)inducesSIRT1expressionwithoutalteringTLXlevelsinT98Ghumanastrocytecellscells[1].TLXagonist3(10µM;0-60min)showsfavorablemicrosomalstability(t1/2=142min)inratlivermicrosomes[1].TLXagonist3(upto10µM;24h)showsnopronouncedcytotoxiceffectsinHEK293cells[1].RealTimeqPCR[1]CellLine:T98GhumanastrocytecellsConcentration:3μMIncubationTime:8h1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:InducedexpressionoftheTLX-regulatedgeneSIRT1butdidnotalterTLXlevels.REFERENCES[1].FaudoneG,etal.DesignofaPotentTLXAgonistbyRationalFragmentFusion.JMedChem.2022;65(3):2288-2296.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021-589559