LY-2562175 Chemical Properties

Boiling point:

740.1±60.0 °C(Predicted)

Density 

1.48±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMF: 20 mg/ml; DMSO: 30 mg/ml; DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml

form 

A crystalline solid

pka

3.43±0.10(Predicted)

LY-2562175 Usage And Synthesis

Description

LY2562175 is a farnesoid X receptor (FXR) agonist (EC₅₀ = 193 nM in a reporter assay). 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.

Uses

LY2562175, is a potent and selective FXR agonist with an EC50 of 193 nM.

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