CP-868388 free base

• CAT Number: I006013
• CAS Number: 702681-67-2
• Molecular Formula: C26H33NO5
• Molecular Weight: 439.54
• Purity: ≥95%
• Synonyms: 2-methyl-2-[3-[(3S)-1-[(4-propan-2-ylphenyl)methoxycarbonyl]piperidin-3-yl]phenoxy]propanoic acid
• InChI: InChI=1S/C26H33NO5/c1-18(2)20-12-10-19(11-13-20)17-31-25(30)27-14-6-8-22(16-27)21-7-5-9-23(15-21)32-26(3,4)24(28)29/h5,7,9-13,15,18,22H,6,8,14,16-17H2,1-4H3,(H,28,29)/t22-/m1/s1
• InChIKey: CSLFIHDRJSTULR-JOCHJYFZSA-N
• SMILES: CC(C)C1=CC=C(C=C1)COC(=O)N2CCCC(C2)C3=CC(=CC=C3)OC(C)(C)C(=O)O

CP-868388 free base is a potent, selective and orally active PPARα agonist with a Ki value of 10.8 nM. CP-868388 free base has little or no affinity for PPARβ (Ki of 3.47 μM) and PPARγ. CP-868388 free base has hypolipidemic and anti-inflammatory actions[1].
CP-868388 (0-1 mM) displays robust and dose-dependent recruitment of SRC-1 (EC50 of 4.7 nM) and PGC-1α peptide[1].
CP-868388 demonstrate robust and selective transcriptional activation of PPARα with an EC50 of 18 nM in HepG2 cells[1].
CP-868388 (0-3 mg/kg; oral gavage; once daily; for 2 days; male B6/CBF1J mice) treatment shows a robust and highly significant decrease in circulating plasma triglycerides. Triglyceride lowering is dose-dependent with the greatest efficacy achieved at the 3.0 mg/kg dose, with triglyceride decreases of ~50%[1].

Reference

[1]. Christopher D Kane, et al. Molecular characterization of novel and selective peroxisome proliferator-activated receptor alpha agonists with robust hypolipidemic activity in vivo. Mol Pharmacol. 2009 Feb;75(2):296-306.
 [Content Brief]