LY2562175

LY2562175 is a farnesoid X receptor (FXR) agonist (EC₅₀ = 193 nM in a reporter assay).¹ It is selective for FXR over the glucocorticoid, androgen, mineralocorticoid, and progesterone receptors in HEK293 cells overexpressing the human receptors (EC₅₀s = >10 µM for all in a radioligand binding assay). LY2562175 increases the interaction between FXR and steroid receptor coactivator 1 (SRC-1) with an EC₅₀ value of 121 nM in a cell-free assay. It reduces plasma triglyceride and total cholesterol levels in LDL receptor-null mice (ED₅₀s = 3.4 and 2 mg/kg, respectively). LY2562175 also decreases plasma LDL and increases HDL levels in Zucker diabetic fatty (ZDF) rats when administered at doses of 3, 10, and 30 mg/kg for nine days.

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1. Genin, M.J., Bueno, A.B., Francisco, J.A., et al. Discovery of 6-(4-{[5-cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl]methoxy}piperidin-1-yl)-1-methyl-1H-indole-3-carboxylic acid: A novel FXR agonist for the treatment of dyslipidemia. J. Med. Chem. 58(24), 9768-9772 (2015).