NS-638是具有阻断Ca²⁺-离子通道性质的非肽类小分子。细胞内阻断由K⁺激活的Ca²⁺浓度升高的IC₅₀值为3.4 μM。

NS-638 is a small nonpeptide molecule with Ca-channel blocking properties. K-stimulated intracellular Ca-elevation is blocked with an IC 50 value of 3.4 μM.

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IC50: 3.4 μM (K-stimulated intracellular Ca-elevation)

NS-638 dose dependently inhibits K-stimulated [45 Ca]-uptake in chick cortical synaptosomes and 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA)- stimulated [H]GABA-release from cultured cortical neurons with IC50 values of 2.3 and 4.3 μM, respectively. K-stimulated intracellular Ca-elevation in cultured cerebellar granule cells is equipotently blocked with an IC50 value of 3.4 μM. At this concentration no effect on Ca-induced contractions in K-depolarized guinea pig taenia coli is observed. NS-638 reversibly blocks N- and L-type Ca-channels in cultured chick dorsal root ganglion cells in the concentration range of 1-30 μM. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. M?ller A, et al. Pharmacological profile and anti-ischemic properties of the Ca(2+)-channel blocker NS-638. Neurol Res. 1995 Oct;17(5):353-60.

In Vitro: DMSO : ≥ 34 mg/mL (104.38 mM)配制储备液