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Tat-NR2B9c
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAS NO:500992-11-0
包装与价格:
包装价格(元)
10 mM * 1 mL in Water电议
1mg电议
5mg电议
10mg电议
25mg电议

产品名称
Tat-NR2Bct
NA-1
产品介绍
Tat-NR2B9c (Tat-NR2Bct; NA-1) 是一种PSD-95的抑制剂,抑制 PSD-95d2 (PSD-95 PDZ domain 2) 和 PSD-95d1 的EC50分别为 6.7 nM 和 670 nM。Tat-NR2B9c 扰乱了 PSD-95/NMDAR 的相互作用,抑制 PSD-95 和 NR2A 和 NR2B 结合的IC50值分别为 0.5 μM 和 8 μM。Tat-NR2B9c 还能抑制神经元一氧化氮合酶 (nNOS)/PSD-95 相互作用,具有神经保护作用。
生物活性

Tat-NR2B9c (Tat-NR2Bct; NA-1) is apostsynaptic density-95 (PSD-95)inhibitor, withEC50values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 withIC50values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy[1][2][5].

IC50& Target

NMDA Receptor

 

nNOS

 

体外研究
(In Vitro)

Tat-NR2B9c is a PSD-95 inhibitor, with an EC50of 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 IC50of ~0.2 μM[1].
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[2].

体内研究
(In Vivo)

Tat-NR2B9c (10 nmol/g, i.v.) reduces infarction volume of male C57BL/6 mice, but has no effect at 3 nM/g[3].

分子量

2518.88

性状

Solid

Formula

C105H188N42O30

CAS 号

500992-11-0

Sequence Shortening

YGRKKRRQRRRKLSSIESDV

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-80°C2 years
-20°C1 year
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

H2O : ≥ 50 mg/mL(19.85 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM0.3970 mL1.9850 mL3.9700 mL
5 mM0.0794 mL0.3970 mL0.7940 mL
10 mM0.0397 mL0.1985 mL0.3970 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:
  • 1.

    Tat-NR2B9c is prepared in saline[4].