| 产品描述： | LDN-212320 is a glutamate transporter EAAT2 activator. It also enhances EAAT2 levels by > 6 fold at concentrations < 5 μM after 24 h |
| 靶点： |
transporter |
| 体外研究： |
LDN/OSU-0212320 enhanced EAAT2 protein levels and glutamate uptake function but did not affect EAAT1 or EAAT3 protein levels and it also increased EAAT2 protein levels in a dose-dependent (EC50: 1.83 ± 0.27 μM) and time-dependent manner. LDN/OSU-0212320 treatment markedly prevented neuronal loss and degeneration, as assessed by MAP2 immunostaining |
| 体内研究： |
After LDN/OSU-0212320(a single i.p.; 40-mg/kg) treatment, EAAT2 protein levels and associated glutamate uptake increased by approximately 1.5- to 2-fold at 2 hours and by approximately 2- to 3-fold between 8 and 24 hours after injection. Even 72 hours after injection, an approximately 1.5-fold increase in EAAT2 protein levels could still be detected (data not shown). LDN/OSU-0212320–induced EAAT2 protein levels and glutamate uptake was dose-dependent |
| 参考文献： |
1. Xing X, et al. Structure-activity relationship study of pyridazine derivatives as glutamate transporter EAAT2 activators. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5774-7. 2. Kong Q, et al. Small-molecule activator of glutamate transporter EAAT2 translation provides neuroprotection. J Clin Invest. 2014 Mar;124(3):1255-67. |
| 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 |
3.408 ml |
17.042 ml |
34.085 ml |
| 5 mM |
0.682 ml |
3.408 ml |
6.817 ml |
| 10 mM |
0.341 ml |
1.704 ml |
3.408 ml |
| 50 mM |
0.068 ml |
0.341 ml |
0.682 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京