S87114 |
LDN-212320 |
| 源叶(MedMol) | 98% |
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- 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： -20℃
- 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
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