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MA-0204 is an agonist of peroxisome proliferator-activated receptor δ (PPARδ).1 It selectively induces reporter gene expression in CV-1 cells expressing human PPARδ (EC50 = 0.4 nM) over CV-1 cells expressing human PPARα or PPARγ (EC50s = 6,990 and >10,000 nM, respectively). MA-0204 increases the expression of mRNA encoding angiopoietin-related protein 4 (ANGPTL4), carnitine palmitoyltransferase 1 (CPT1), and pyruvate dehydrogenase kinase 4 (PDHK4) in primary myoblasts from a patient with Duchenne muscular dystrophy (DMD) in a concentration-dependent manner. In vivo, MA-0204 (30 or 100 mg/kg) increases the expression of mRNA encoding Pdhk4 in the skeletal muscle of mice.
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1. Selective PPAR# modulators improve mitochondrial function: Potential treatment for duchenne muscular dystrophy (DMD). ACS Med. Chem. Lett. (2018).