| 产品描述： | WAY-213613 is a potent and selective human EAAT2 inhibitor. WAY-213613 has potent EAAT2 inhibitory activity with an IC50 value of 85 nM. WAY-213613 can be used for the research of central nervous system |
| 靶点： |
EAAT2;transporter |
| 体外研究： |
WAY-213613 (0-100 μM) has inhibitory activity for human EAAT1, EAAT2 and EAAT3 subtype with IC50 values of 5004 nM, 85 nM and 3787 nM, respectively. WAY-213613 (3, 30, 300 nM) has the inhibitory effect on synaptosomal L-[3H] glutamate uptake with Ki values of 15 nM, 41 nM and 55 nM in the presence of 3, 30 and 300 nM, respectively. WAY-213613 (0-100 μM) produces a concentration-dependent block of glutamate-induced currents in EAAT1-, EAAT2- or EAAT3-injected oocytes, with IC50 values of 48, 0.13 and 4.0 μM, respectively. WAY-213613 (0.5–50 μM) exhibits good selectivity over ionotropic receptors and EAAT2 and potent activity toward blocking NMDA-stimulated responses |
| 参考文献： |
1. Dunlop J, et al. Characterization of novel aryl-ether, biaryl, and fluorene aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinity glutamate transporter EAAT2. Mol Pharmacol. 2005 Oct;68(4):974-82. Epub 2005 Jul 13. 2. Simmons DA, et al. A small molecule p75NTR ligand, LM11A-31, reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression. PLoS One. 2014 Aug 25;9(8):e102136. |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.214 ml |
11.071 ml |
22.141 ml |
| 5 mM |
0.443 ml |
2.214 ml |
4.428 ml |
| 10 mM |
0.221 ml |
1.107 ml |
2.214 ml |
| 50 mM |
0.044 ml |
0.221 ml |
0.443 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