Tat-NR2B9c (Synonyms:Tat-NR2Bct; NA-1)
目录号 : KM12321 CAS No. : 500992-11-0

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。

规格 价格 是否有货 数量
1mg
In-stock
5mg
In-stock
10mg
In-stock
25mg
In-stock

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生物活性

Tat-NR2B9c (Tat-NR2Bct; NA-1) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values 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 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy.

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.

分子式
C105H188N42O30
分子量
2518.88
CAS号
500992-11-0
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -80°C 2 years
-20°C 1 year
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

H2O : 100 mg/mL (39.70 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.3970 mL 1.9850 mL 3.9700 mL
5 mM 0.0794 mL 0.3970 mL 0.7940 mL
10 mM 0.0397 mL 0.1985 mL 0.3970 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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

 
科研文献
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