An FXR agonist (EC50 = 193 nM in a reporter assay); selective for FXR over the glucocorticoid

LY2562175 – 10 mg

Brand:
Cayman
CAS:
1103500-20-4
Storage:
-20
UN-No:
Non-Hazardous - /

LY2562175 is a farnesoid X receptor (FXR) agonist (EC50 = 193 nM in a reporter assay).{48622} 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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Description

An FXR agonist (EC50 = 193 nM in a reporter assay); 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); increases the interaction between FXR and SRC-1 (EC50 = 121 nM in a cell-free assay); reduces plasma triglyceride and total cholesterol levels in LDL receptor-null mice (ED50s = 3.4 and 2 mg/kg, respectively); decreases plasma LDL and increases HDL levels in ZDF rats at 3, 10, and 30 mg/kg for nine days

Formal name: 6-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-4-isoxazolyl]methoxy]-1-piperidinyl]-1-methyl-1H-indole-3-carboxylic acid

Synonyms: 

Molecular weight: 540.4

CAS: 1103500-20-4

Purity: ≥95%

Formulation: A crystalline solid

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