FXR-agonist-15-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEFXRagonist15Cat.No.:HY-179703CASNo.:2991276-14-1分⼦式:C₂₄H₂₂Cl₂FNO₅S分⼦量:526.4作⽤靶点:FXR作⽤通路:MetabolicEnzyme/Protease储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性FXRagonist15⼀种选择性、强效且有⼝服活性的法尼酯X受体(FXR)激动剂，其EC50值为0.76μM。FXRagonist15对其他核受体，包括LXRα/β、PXR、PPARα/β/γ和THR-β⽆明显激活作⽤，其EC50均⼤于10μM。FXRagonist15可减轻脂变性、⼩叶炎症、肝细胞⽓球样变和肝纤维化。FXRagonist15可⽤于⾮精性脂性肝炎(NASH)的研究。体内研究FXRagonist15(Compound19)(20mg/kg,i.g.,perdayfor4weeks)alleviatesNASHbyreducingliversteatosis,inflammation,andfibrosisinWD+CCl4(HY-Y0298)-inducedmiceNASHmodels[1].FXRagonist15(500mg/kg,p.o.,oncedailyfor10days)causesnomousedeathorabnormalbehavior,showsnosignificantabnormalitiesinserumliverandkidneyfunctionindices(AST,ALT,ALP,creatinine,urea)andbloodlipidindices(TG,TC),exhibitsnoacutetoxicdamagetomajororgans,andhasgoodsafetyinICRmice[1].AnimalModel:WD+CCl4-inducedmiceNASHmodels(C57BL/6,8weeks)[1]Dosage:20mg/kgAdministration:Orallygavage,perdayfor4weeksResult:Reducedhepaticlipiddroplets,NAFLDactivityscore(NAS),andlevelsoftriacylglycerol(TG)andtotalcholesterol(TC).Decreasedfibroticmarkers(α-SMA,hydroxyproline)andactivatedtheFXRpathway.UpregulatedSHP,BSEP,andOSTβ,whiledownregulatedCYP7A1.REFERENCES1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].WangW,etal.Design,synthesis,andbiologicalstudiesofnovelsulfonamidederivativesasfarnesoidXreceptoragonists.EurJMedChem.2023;258:115614.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;02