CP-868388 free base (CP-868388) is an orally active, potent and selective PPARα agonist with hypolipidemic and anti-inflammatory activity for the study of dyslipidemia.

PPARα (human):10.8 nM (Ki), SRC-1:4.7 nM (EC50), PPARγ (human):3.47 μM (Ki), HepG2 cells:18 nM (EC50)

The compound CP-868388, at concentrations ranging from 0-1 mM, exhibits strong and dose-dependent recruitment of SRC-1, with an EC50 of 4.7 nM, as well as the PGC-1α peptide[1]. Additionally, CP-868388 demonstrates potent and selective transcriptional activation of PPARα, showing an EC50 of 18 nM in HepG2 cells[1].

In male B6/CBF1J mice, treatment with CP-868388 (oral gavage; once daily; for 2 days) at doses ranging from 0-3 mg/kg results in a robust and highly significant decrease in circulating plasma triglycerides. The dose-dependent effect is observed, with the highest efficacy achieved at the 3.0 mg/kg dose, leading to a reduction of approximately 50% in triglyceride levels[1].