LY-2562175

Research use only, not for human use.

LY-2562175 (LY2562175, LY 2562175) is a novel potent, selective, partial FXR agonist with EC50 of 193 nM.

LY-2562175 (LY2562175, LY 2562175) is a novel potent, selective, partial FXR agonist with EC50 of 193 nM; does not promote transcriptional activation of other nuclear receptor, such as GR, PR, MR and AR (EC50>10 uM); lowers LDL and triglycerides while raising HDL in preclinical species.Dyslipidemia Preclinical.

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

LY2562175 causes a dose-dependent decrease in serum cholesterol and serum triglycerides. 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 control group. The ED50 for serum cholesterol is determined to be 2 and 3.4 mg/kg for serum triglycerides. Treatment of female ZDF rats with LY2562175 results in a dose dependent lowering of plasma triglycerides in the fasted and nonfasted states. When administered as a fixed dose combination with BRL49653, LY2562175 further lowers fasted and nonfasted plasma triglycerides. FPLC fractionation of the lipoproteins reveals that LY2562175 treatment results in a reduction in vLDL-C and a dramatic increase in HDL-c in this animal model.

LY2562175 | LY 2562175

Metabolic Enzyme/Protease

FXR

FXR

Cardiovascular Disease

Dyslipidemia

1103500-20-4

540.441

C28H27Cl2N3O4

>98% (HPLC)

DMSO : 62.5 mg/mL 115.65 mM; H2O : < 0.1 mg/mL

O=C(C1=CN(C)C2=C1C=CC(N3CCC(OCC4=C(C5CC5)ON=C4C6=C(Cl)C=CC=C6Cl)CC3)=C2)O

6-(4-((5-cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl)methoxy)piperidin-1-yl)-1-methyl-1H-indole-3-carboxylic acid

(-20℃)

With Ice Pack

≥ 2 years