MA-0204 是一种高选择性,可口服的过氧化物酶体增殖物激活受体 δ (PPARδ) 调节剂,对于人,小鼠和大鼠 PPARδ 的EC50分别为 0.4、7.9 和 10 nM。它有用于 Duchene 肌营养不良症 (DMD) 的研究潜力。
产品描述
MA-0204 is a highly selective and orally available peroxisome proliferator-activated receptor δ (PPARδ) modulator (EC50s: 0.4 nM, 7.9 nM and 10 nM for human, mouse and rat PPARδ, respectively). It is a potential treatment for Duchene Muscular Dystrophy (DMD).
体外活性
MA-0204 is >10,000-fold selective for activation of PPARδ over PPARα and PPARγ receptors. MA-0204 (1.2-12 nM) improves fatty acid oxidation in DMD patient muscle myoblasts mice. MA-0204 shows high protein binding to mouse plasma, good permeability, and low potential for efflux. C.
体内活性
In the muscle, PPARδ (30, 100 mg/kg) enhances target gene transcription.
Cas No.
2095128-17-7
分子式
C25H27F3N2O4
分子量
476.49
储存和溶解度
DMSO:40 mg/mL (83.95 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years