| Bioactivity | 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]. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| In Vivo | PPARδ (30, 100 mg/kg) increases target gene transcription in the muscle[1]. | ||||||||||||
| Name | MA-0204 | ||||||||||||
| CAS | 2095128-17-7 | ||||||||||||
| Formula | C25H27F3N2O4 | ||||||||||||
| Molar Mass | 476.49 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |