Pricing updated 2019-07-17. Prices are subject to change without notice.
Tropifexor is an agonist of farnesoid X receptors (FXR).1 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).2
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Tully, D.C., Rucker, P.V., Chianelli, D., et al. Discovery of tropifexor (LJN452), a highly potent non-
Laffitte, B., Hernandez, E., Kim, Y., et al. THU-