| 产品描述: | ML-SA5 is a potent TRPML1 cation channel agonist that activates the entire endosomal TRPML1 (ML1) current in DMD myocytes with an EC50 of 285 nM and is more potent than ML-SA1. ML-SA5 has anticancer activity and can inhibit tumour growth |
| 靶点: |
TRP Channel;Autophagy |
| 体外研究: |
ML-SA5(1-100 μM, 24 h) has some cell-targeting specificity and induces substantial cell death in M12 and MeWo cells, but fully preserves normal melanocytes. It also causes a loss of mitochondrial membrane potential in M12 cells |
| 体内研究: |
ML-SA5 (i.p., 2-5 mg/kg, daily, 2 weeks) reduces muscle necrosis in MDX mice by more than 70% and reduces central nucleated fibers, suggesting that ML-SA5 can improve muscle atrophy in mdx mice in vivo by promoting myosin repair, but has no effect in ML1 knockout mice. Moreover, ML-SA5 reduces skeletal and cardiac muscle damage in mdx mice through ML1 upregulation |
| 参考文献: |
1. Wanlu Du, et al. Lysosomal Zn2+ release triggers rapid, mitochondria-mediated, non-apoptotic cell death in metastatic melanoma. Cell Rep. 2021 Oct 19;37(3):109848. 2. Lu Yu, et al. Small-molecule activation of lysosomal TRP channels ameliorates Duchenne muscular dystrophy in mouse models. Sci Adv. 2020 Feb 7;6(6):eaaz2736. |
| 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 |
2.183 ml |
10.917 ml |
21.835 ml |
| 5 mM |
0.437 ml |
2.183 ml |
4.367 ml |
| 10 mM |
0.218 ml |
1.092 ml |
2.183 ml |
| 50 mM |
0.044 ml |
0.218 ml |
0.437 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。 |