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Tat-NR2B9c TFA
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:1834571-04-8
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品名称
Tat-NR2Bct TFA
NA-1 TFA
产品介绍
Tat-NR2B9c TFA (Tat-NR2Bct TFA) 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 TFA 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 TFA 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 TFA (Tat-NR2Bct TFA) is a postsynaptic 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 TFA 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 TFA also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy[1].

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 nmol/g[3].

分子量

2632.90

性状

Solid

Formula

C105H188N42O30.C2HF3O2

CAS 号

1834571-04-8

Sequence Shortening

YGRKKRRQRRRKLSSIESDV

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Protect from light, stored under nitrogen

Powder-80°C2 years
-20°C1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
In Vitro: 

H2O : ≥ 50 mg/mL(18.99 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM0.3798 mL1.8990 mL3.7981 mL
5 mM0.0760 mL0.3798 mL0.7596 mL
10 mM0.0380 mL0.1899 mL0.3798 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 (protect from light, stored under nitrogen)。-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:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 100 mg/mL (37.98 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。