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OBESITY RESEARCH SOLUTIONSClofibrate is a selective agonist of peroxisome proliferator-activated receptor α (PPARα).1 In a transactivation assay, clofibrate exhibits EC50 values of 50 and 55 µM for murine and human PPARα, respectively. It also binds to PPARγ but with 10-fold less affinity and is inactive at PPARδ at concentrations up to 100 µM. Formulations containing clofibrate have been used to treat dyslipidemia and cardiovascular disease.
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1. The PPARs: From orphan receptors to drug discovery. J. Med. Chem. 43(4), 527-550 (2000).