Tropifexor

Tropifexor is an agonist of farnesoid X receptors (FXR). It enhances the interaction between the human FXR ligand binding domain and the steroid receptor coactivator 1 (SRC-1) peptide in a homogeneous time-resolved fluorescence (HTRF) coactivator interaction assay (EC50 = 0.2 nM). It increases expression of the FXR target genes BSEP and SHP and decreases expression of CPY8B1 in rat liver in a dose-dependent manner, as well as increases expression of SHP and FGF15 in rat ileum. Tropifexor (0.3 mg/kg) reduces triglyceride levels by 79% in rat serum. It reduces fibrosis, inflammation, and steatosis in a mouse model of nonalcoholic steatohepatitis (NASH).Formal Name: 2-[(3-endo)-3-[[5-cyclopropyl-3-[2-(trifluoromethoxy)phenyl]-4-isoxazolyl]methoxy]-8-azabicyclo[3.2.1]oct-8-yl]-4-fluoro-6-benzothiazolecarboxylic acid. CAS Number: 1383816-29-2. Synonyms: LJN452. Molecular Formula: C29H25F4N3O5S. Formula Weight: 603.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 10 mg/ml. lambdamax: 313 nm. SMILES: FC1=C2C(SC(N3[C@H]4CC[C@@H]3C[C@H](OCC5=C(C6CC6)ON=C5C7=CC=CC=C7OC(F)(F)F)C4)=N2)=CC(C(O)=O)=C1. InChi Code: InChI=1S/C29H25F4N3O5S/c30-21-9-15(27(37)38)10-23-25(21)34-28(42-23)36-16-7-8-17(36)12-18(11-16)39-13-20-24(35-41-26(20)14-5-6-14)19-3-1-2-4-22(19)40-29(31,32)33/h1-4,9-10,14,16-18H,5-8,11-13H2,(H,37,38)/t16-,17+,18+. InChi Key: VYLOOGHLKSNNEK-PIIMJCKOSA-N.