LY2562175

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.Formal Name: 6-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-4-isoxazolyl]methoxy]-1-piperidinyl]-1-methyl-1H-indole-3-carboxylic acid. CAS Number: 1103500-20-4. Molecular Formula: C28H27Cl2N3O4. Formula Weight: 540.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml. lambdamax: 244 nm. SMILES: CN1C=C(C(O)=O)C2=CC=C(N3CCC(OCC4=C(C5CC5)ON=C4C6=C(Cl)C=CC=C6Cl)CC3)C=C21. InChi Code: InChI=1S/C28H27Cl2N3O4/c1-32-14-20(28(34)35)19-8-7-17(13-24(19)32)33-11-9-18(10-12-33)36-15-21-26(31-37-27(21)16-5-6-16)25-22(29)3-2-4-23(25)30/h2-4,7-8,13-14,16,18H,5-6,9-12,15H2,1H3,(H,34,35). InChi Key: RPVDFHPBGBMWID-UHFFFAOYSA-N.