MA-0204

MA-0204 is a potent, highly selective and orally available peroxisome proliferator activated receptor δ (PPARδ) modulator with EC50s of 0.4 nM, 7.9 nM and 10 nM for human, mouse and rat PPARδ, respectively. Potential treatment for Duchene Muscular Dystrophy (DMD)[1].

Signaling Pathways >> Cell Cycle/DNA Damage >> PPAR

Research Areas >> Metabolic Disease

PPARδ:0.4 nM (EC50, in human)

PPARδ:7.9 nM (EC50, in mouse)

PPARδ:10 nM (EC50, in rat)

MA-0204 is >10,000-fold selective for activation of PPARδ over PPARα and PPARγ receptors. 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.

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