N-Desmethyl-Apalutamide-15N-d4-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEN-Desmethyl-Apalutamide-15N,d4Cat.No.:HY-135331S分⼦式:C₂₀H₉D₄F₄N₄₁₅NO₂S分⼦量:468.43作⽤靶点:Isotope-LabeledCompounds;AndrogenReceptor;CytochromeP450作⽤通路:Others;VitaminDRelated/NuclearReceptor;MetabolicEnzyme/Protease储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性N-Desmethyl-Apalutamide-15N,d415N和氚代标记的N-Desmethyl-Apalutamide(HY-135331)。N-DesmethylApalutamideApalutamide的活性代谢产物，⼀种低活性的雄激素受体拮抗剂，其作⽤⼒是Apalutamide活性的三分之⼀。N-DesmethylApalutamide的形成主由CYP2C8和CYP3A4介导。N-DesmethylApalutamide中等⾄强的CYP3A4和CYP2B6诱导剂，并具有优异的⾎浆蛋⽩结合浓度。REFERENCES[1].Pérez-RuixoC,etal.PopulationPharmacokineticsofApalutamideanditsActiveMetaboliteN-Desmethyl-ApalutamideinHealthyandCastration-ResistantProstateCancerSubjects.ClinPharmacokinet.2019Aug20.[2].SmithMR,etal.Phase2StudyoftheSafetyandAntitumorActivityofApalutamide(ARN-509),aPotentAndrogenReceptorAntagonist,intheHigh-riskNonmetastaticCastration-resistantProstateCancerCohort.EurUrol.2016May6.pii:S0302-2838(16)30133[3].MayMB,etal.Apalutamide:Anewagentinthemanagementofprostatecancer.JOncolPharmPract.2019Dec;25(8):1968-1978.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792ax:021