MA-0204 is a potent, highly selective PPARδ modulator with EC50s of 0.4, 7.9 and 10 nM for human, mouse and rat PPARδ, respectively. Potential treatment for Duchene Muscular Dystrophy (DMD) [1].
MA-0204 is >10,000-fold selective for activation of PPARδ over PPARα and PPARγ receptors. It has EC50s of 6,990 nM and more than 100,000 nM for human PPARα and PPARγ, respectively. MA-0204 exhibits high protein binding to mouse plasma, good permeability and low potential for efflux. C[1].MA-0204 (1.2-12 nM) improves fatty acid oxidation in DMD patient muscle myoblasts mice[1].MA-0204 (0.04-40 nM) engages target gene expression in DMD patient muscle myoblasts[1].
PPARδ (30, 100 mg/kg) increases target gene transcription in the muscle[1].
[1]. Lagu B, et al. Selective PPARδ Modulators Improve Mitochondrial Function: Potential Treatment for Duchenne Muscular Dystrophy (DMD). ACS Med Chem Lett. 2018 Jul 31;9(9):935-940.