耗材描述
Tat-NR2B9c
产品活性: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。
产品来源: https://www.medchemexpress.cn/Tat-NR2B9c.html
研究领域:Membrane Transporter/Ion Channel | Neuronal Signaling | Immunology/Inflammation
作用靶点:iGluR | NO Synthase
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.
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.
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