MA-0204 |
カタログ番号GC19450 |
MA-0204 は、ヒト、マウス、ラットの PPARδ に対してそれぞれ 0.4 nM、7.9 nM、10 nM の EC50 を持つ、強力で選択性の高い経口投与可能なペルオキシソーム増殖因子活性化受容体δ (PPARδ) モジュレーターです。
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Cas No.: 2095128-17-7
Sample solution is provided at 25 µL, 10mM.
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.
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