Formulation: A crystalline solid
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
Purity: ≥98%
Formula Markup: C29H25F4N3O5S
Formula Weight: 603,6
Shelf life (days): 1460
CAS Number: 1383816-29-2
Notes: Tropifexor is an agonist of farnesoid X receptors (FXR).{48126} 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).{48127}
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