化合物NS 638 T3543

Product Introduction
Bioactivity


英文名: NS-638

描述: NS-638 是一种 Ca2+ 通道阻滞剂，可阻断 K+ 刺激的细胞内 Ca2+ 升高，IC50值为3.4 μM。

细胞实验: NS-638 is prepared in 1% DMSO and 1% ethanol. The effect of NS-638 on neuronal Ca2+-channels is evaluated using whole cell patch clamp techniques[1].

体外活性: NS-638 dose-dependently inhibits K+-stimulated [45 Ca2+]-uptake in chick cortical synaptosomes and 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA)- stimulated [3H]GABA-release from cultured cortical neurons (IC50: 2.3 and 4.3 μM), respectively. K+-stimulated intracellular Ca2+-elevation in cultured cerebellar granule cells is equipotently blocked (IC50: 3.4 μM). At this concentration, no effect on Ca2+-induced contractions in K+-depolarized guinea pig taenia coli is observed. NS-638 reversibly blocks N- and L-type Ca2+-channels in cultured chick dorsal root ganglion cells (1-30 μM).

体内活性: In the mouse middle cerebral artery occlusion model, NS-638 administered (50 mg/kg, i.p.) at 1 h and 6 h post-ischemia, and once a day for the next two days, results in a 48% reduction in total infarct volume. It does not show protection against ischemic neuronal damage in the gerbil model of bilateral carotid artery occlusion.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 55 mg/mL (168.86 mM)


关键字: Ca channels | Inhibitor | Calcium Channel | inhibit | NS638 | Ca2+ channels | NS-638

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