Cas No.: | 2095128-17-7 |
Chemical Name: | (3R)-3-Methyl-6-[2-[[5-methyl-2-[4-(trifluoromethoxy)phenyl]imidazol-1-yl]methyl]phenoxy]hexanoic acid |
Synonyms: | (R)-3-methyl-6-(2-((5-methyl-2-(4-(trifluoromethoxy)phenyl)-1H-imidazol-1-yl)methyl)phenoxy)hexanoic acid;(3R)-3-Methyl-6-[2-[[5-methyl-2-[4-(trifluoromethoxy)phenyl]imidazol-1-yl]methyl]phenoxy]hexanoic ac;MA-0204 |
SMILES: | FC(OC1C([H])=C([H])C(=C([H])C=1[H])C1=NC([H])=C(C([H])([H])[H])N1C([H])([H])C1=C([H])C([H])=C([H])C([H])=C1OC([H])([H])C([H])([H])C([H])([H])[C@@]([H])(C([H])([H])[H])C([H])([H])C(=O)O[H])(F)F |
Formula: | C25N2O4F3H27 |
M.Wt: | 476.4881 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | 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]. |
Target: | PPARδ:0.4 nM (EC50, in human) PPARδ:7.9 nM (EC50, in mouse) PPARδ:10 nM (EC50, in rat) |
In Vivo: | PPARδ (30, 100 mg/kg) increases target gene transcription in the muscle[1]. |
In Vitro: | 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]. |
References: | [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. |