LY2562175 是一种有效的选择性 FXR 激动剂，其EC50值为 193 nM。

LY2562175 is an effective and selective FXR agonist (EC50: 193 nM).

LY2562175 boosts transcriptional activation of human FXR in a cell-based co-transfection assay (EC50: 193 nM) and it also promotes the recruitment of a peptide from the nuclear receptor interaction domain of the coactivator SRC-1 (a relative EC50: 121 nM). It has 93.5% efficacy as compare to GW4064.

LY2562175 induces a dose-dependent decrease in serum cholesterol and serum triglycerides. LY2562175(female ZDF rats) treatment, causes a dose-dependent lowering of plasma triglycerides in the fasted and nonfasted states. LY2562175 further lowers fasted and nonfasted plasma triglycerides when administered as a fixed-dose combination with BRL49653. At a dose of 10 mg/kg, the decrease in cholesterol with LY2562175 is 80% below vehicle-treated animals, and the decrease in serum triglycerides is 76% from the control group. The ED50 for serum cholesterol is determined to be 2 and 3.4 mg/kg for serum triglycerides. FPLC fractionation of the lipoproteins shows that LY2562175 treatment causes a reduction in vLDL-C and a dramatic increase in HDL-c in this animal model.

1103500-20-4

C28H27Cl2N3O4

540.44

H2O:< 0.1 mg/mL (insoluble)
DMSO:62.5 mg/mL (115.65 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years