Peroxisome proliferator-activated receptor-α (PPARα) is a ligand-activated transcription factor involved in the regulation of lipid homeostasis. Activation of PPARα results in expression of a variety of genes, particularly those involved in fatty acid β-oxidation, binding, and transport. GW 7647 is a potent, selective agonist of human and murine PPARα4 It activates human PPARα, PPARγ, and PPARδ with EC50 values of 0.006, 1.1 and 6.2 µM, respectively, in a GAL4-PPAR binding assay. Similar EC50 values of 0.001, 1.3, and 2.9 were observed with the murine receptors. GW 7647 lowered triglycerides 93% and 60% in fat-fed hamsters and rats, respectively, at a dose of 3 mg/kg.
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