Tat-NR2B9c|500992-11-0|(Tat-NR2Bct; NA-1)-陌孚医药/Medlife

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Tat-NR2B9c (Synonyms: Tat-NR2Bct; NA-1)

目录号: PL07833

CAS No. :500992-11-0

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中文名称	Tat-NR2B9c
中文别名	L-酪氨酰甘氨酰-L-精氨酰-L-赖氨酰-L-赖氨酰-L-精氨酰-L-精氨酰-L-谷氨酰胺酰-L-精氨酰-L-精氨酰-L-精氨酰-L-赖氨酰-L-亮氨酰-L-丝氨酰-L-丝氨酰-L-异亮氨酰-L-alpha-谷氨酰-L-丝氨酰-L-alpha-天冬氨酰-L-缬氨酸;Tat-NR2B9c
英文名称	Tat-NR2B9c
英文别名	Tat-NR2B9c;Nerinetide;D45TI2TWMA;NA-1;FN023;Nerinetide [USAN];Tat NR2B9c;WHO 10857;L-tyrosylglycyl-L-arginyl-L-lysyl-L-lysyl-L-arginyl-L-arginyl-L- glutaminyl-L-arginyl-L-arginyl-L-arginyl-L-lysyl-L-leucyl-L-seryl-L-seryl-L-isoleucyl-L-alpha-glutamyl-L-seryl-L-alpha-aspartyl-L-valine;L-Valine, L-tyrosylglycyl-L-arginyl-L-lysyl-L-lysyl-L-arginyl-L-arginyl-L- glutaminyl-L-arginyl-L-arginyl-L-arginyl-L-lysyl-L-leucyl-L-seryl-L-seryl-L-isoleucyl-L-alpha-glutamyl-L-seryl-L
Cas No.	500992-11-0
分子式	C₁₀₅H₁₈₈N₄₂O₃₀
分子量	2518.88
包装储存	Sealed storage, away from moisturePowder -80°C 2 years；-20°C 1 year

产品详情	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 a postsynaptic density-95 (PSD-95) inhibitor, with EC 50 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 IC 50 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.
性状	Solid
IC50 & Target[1][2]	NMDA Receptor nNOS
体外研究(In Vitro)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Sealed storage, away from moisturePowder -80°C 2 years；-20°C 1 year
SequenceShortening	YGRKKRRQRRRKLSSIESDV
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.

溶解度数据	In Vitro: H₂O : ≥ 50 mg/mL (19.85 mM)配制储备液

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