NS-638

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种非肽钙通道阻滞剂，剂量依赖性地抑制 AMPA 刺激的 [3H]GABA 释放。

A nonpeptide calcium channel blocker that dose dependently inhibits AMPA-stimulated [3H]GABA-release from cultured cortical neurons with IC50 of 4.3 uM; blocks K(+)-stimulated intracellular Ca(2+)-elevation in cultured cerebellar granule cells with IC50 of 3.4 uM, reversibly blocks N- and L-type Ca(2+)-channels in cultured chick dorsal root ganglion cells (1-30 uM); exhibits anti-ischemic properties in vivo.

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 with IC50 values of 2.3 and 4.3 μM, respectively. K+-stimulated intracellular Ca2+-elevation in cultured cerebellar granule cells is equipotently blocked with an IC50 value of 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 in the concentration range of 1-30 μM.

In the mouse middle cerebral artery occlusion model, NS-638 administered i.p. (50 mg kg-1) 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.

NS638 | NS 638

GPCR/G Protein

Calcium Channel

K+-stimulatedintracellularCa2+-elevation

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150493-34-8

325.7161496

C15H11ClF3N3

>98% (HPLC)

DMSO: ≥ 34 mg/mL

FC(C1=CC=C2C(N=C(N)N2CC3=CC=C(Cl)C=C3)=C1)(F)F

1H-Benzimidazol-2-amine, 1-[(4-chlorophenyl)methyl]-5-(trifluoromethyl)-

(-20℃)

With Ice Pack

≥ 2 years