| 产品描述: | 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) |
| 靶点: |
PPARδ:0.4 nM (EC50, in human);PPARδ:7.9 nM (EC50, in mouse);PPARδ:10 nM (EC50, in rat);PPAR |
| 体外研究: |
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. MA-0204 (1.2-12 nM) improves fatty acid oxidation in DMD patient muscle myoblasts mice. MA-0204 (0.04-40 nM) engages target gene expression in DMD patient muscle myoblasts |
| 体内研究: |
PPARδ (30, 100 mg/kg) increases target gene transcription in the muscle |
| 参考文献: |
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. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.099 ml |
10.493 ml |
20.987 ml |
| 5 mM |
0.42 ml |
2.099 ml |
4.197 ml |
| 10 mM |
0.21 ml |
1.049 ml |
2.099 ml |
| 50 mM |
0.042 ml |
0.21 ml |
0.42 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |