LMB763 is a partial agonist of the farnesoid X receptor (FXR; EC50 = 7 nM).1 It is selective for FXR over a panel of enzymes, ion channels, nuclear receptors, and G protein-coupled receptors, including the androgen receptor, estrogen receptor α (ERα), and G protein-coupled bile acid receptor 1 (GPBAR1; EC50s = >30, >30, and >80 ?M, respectively). LMB763 induces expression of the FXR target genes encoding the bile salt export pump and short heterodimer partner in isolated rat hepatocytes in a concentration-dependent manner. It decreases non-alcoholic fatty liver disease (NAFLD) scores and liver fibrosis in a rat model of non-alcoholic steatohepatitis (NASH).
1.Chianelli, D., Rucker, P.V., Roland, J., et al.Nidufexor (LMB763), a novel FXR modulator for the treatment of nonalcoholic steatohepatitis (NASH)J. Med. Chem.63(8)3868-3880(2020)