| 产品名称: |
nerinetide |
| 规格或纯度: |
Moligand™ |
| 靶点: |
NMDA Receptor;nNOS |
| 体外研究: |
Tat-NR2B9c is a PSD-95 inhibitor, with an EC50 of 6.7 nM for PSD-95d2, representing a >100-fold higher affinity for this domain than for PSD-95d1 (EC50, 0.67 μM). Tat-NR2B9c inhibits NMDAR2A, NMDAR2B, and NMDAR2C binding to PSD-95, with IC50s of 0.5 μM, ∼8 μM, and 0.75 μM, respectively. Tat-NR2B9c also blocks the interaction between PSD-95 and nNOS with an IC50 of ∼0.2 μM. Tat-NR2B9c reduces association of PSD-95 with GluN2B by ∼50% in the YAC128 striatum, decreases NMDA-induced p38 activation in YAC128 striatal tissue, but shows no effect on the NMDA-induced JNK activation |
| 体内研究: |
Tat-NR2B9c (10 nmol/g, i.v.) reduces infarction volume of male C57BL/6 mice, but has no effect at 3 nM/g |
| 参考文献: |
1. Cui H, et al. PDZ protein interactions underlying NMDA receptor-mediated excitotoxicity and neuroprotection by PSD-95 inhibitors. J Neurosci. 2007 Sep 12;27(37):9901-15. 2. Fan J, et al. P38 MAPK is involved in enhanced NMDA receptor-dependent excitotoxicity in YAC transgenic mouse model of Huntington disease. Neurobiol Dis. 2012 Mar;45(3):999-1009. 3. Teves LM, et al. Efficacy of the PSD95 inhibitor Tat-NR2B9c in mice requires dose translation between species. J Cereb Blood Flow Metab. 2016 Mar;36(3):555-61. 4. Jing Fan, et al. N-methyl-D-aspartate Receptor Subunit- And Neuronal-Type Dependence of Excitotoxic Signaling Through Post-Synaptic Density 9. J Neurochem. 2010 Nov;115(4):1045-56. |
| 溶解性: |
Soluble in H2O |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
0.397 ml |
1.985 ml |
3.97 ml |
| 5 mM |
0.079 ml |
0.397 ml |
0.794 ml |
| 10 mM |
0.04 ml |
0.199 ml |
0.397 ml |
| 50 mM |
0.008 ml |
0.04 ml |
0.079 ml |
|
| 注意: |
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