CP 775,146 is an agonist of peroxisome proliferator-activated receptor α (PPARα) that selectively binds to PPARα (K = 24.5 nM) over PPARβ and PPARγ (Ks = >10,000 nM). CP 775,146 induces PPARα transcriptional activity in a reporter assay (ECs = 57 and 284 nM for human and rat receptors, respectively, expressed in HepG2 cells). It decreases plasma triglyceride levels in mice by 73% when administered at a dose of 2 mg/kg per day for two days.