LY2562175

• CAT Number: I007808
• CAS Number: 1103500-20-4
• Molecular Formula: C28H27Cl2N3O4
• Molecular Weight: 540.441
• Purity: ≥95%
• Target: FXR agonist
• Solubility: Soluble in DMSO, not in water
• Storage: 0 - 4°C for short term , or -20°C for long term.
• IUPAC Name: 6-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]piperidin-1-yl]-1-methylindole-3-carboxylic acid
• InChI: 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)
• InChIKey: RPVDFHPBGBMWID-UHFFFAOYSA-N
• SMILES: CN1C=C(C2=C1C=C(C=C2)N3CCC(CC3)OCC4=C(ON=C4C5=C(C=CC=C5Cl)Cl)C6CC6)C(=O)O

LY2562175 (CAT: I007808) is a potent and selective agonist of the farnesoid X receptor (FXR) in vitro. It demonstrates robust lipid-modulating properties, effectively lowering LDL cholesterol and triglyceride levels while increasing HDL cholesterol in preclinical studies. LY2562175 exhibits favorable pharmacokinetic properties, supporting once-daily dosing in humans. It activates the transcriptional activity of human FXR in cell-based assays with an EC50 (half-maximal effective concentration) of approximately 193 nM. The promising preclinical results of LY2562175 have led to its advancement into clinical evaluation as a potential therapeutic agent for various lipid-related disorders.

Reference

1:Genin MJ, Bueno AB, Agejas Francisco J, Manninen PR, Bocchinfuso WP, Montrose-Rafizadeh C, Cannady EA, Jones TM, Stille JR, Raddad E, Reidy C, Cox A, Michael MD, Michael LF. Discovery of 6-(4-{[5-Cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl]methoxy}piperidin-1-yl)-1-methyl-1H-indole-3-carboxylic Acid: A Novel FXR Agonist for the Treatment of Dyslipidemia. J Med Chem. 2015 Dec 2. [Epub ahead of print] PubMed PMID:26568144.