CP-775146

CP-775146 is a selective PPARα agonist (K_i of 24.5 nM) that binds strongly to the PPARα ligand. CP-775146 has no observable affinity for PPARβ and PPARγ.CP-775146 shows hypolipidemic activity. CP-775146 efficiently alleviates obesity-induced liver damage, prevents lipid accumulation by activating the liver fatty acid β-oxidation pathway^[1][2]. In Vitro:CP-775146 induces PPARα transcriptional activity in a reporter assay, the EC₅₀s of 57 nM and 284 nM for human and rat receptors, respectively, expressed in HepG2 cells^[1] In Vivo:CP-775146 (0.1-0.3 mg/kg; i.p.; daily; for 3 days) efficiently alleviates obesity-induced liver damage, prevents lipid accumulation by activating the liver fatty acid β-oxidation pathway, and regulates the expression of genes that control brown fat-like pathway in eWAT^[2].