CAS:448895-37-2NS-1643

NS-1643 is a potent human ether-a-go-go related gene (hERG) KV11.1 channel activator with EC50 of 10.5 μM.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

448895-37-2

储存条件

分子式

C15H10F6N2O3

运输

蓝冰

分子量

380.24

别名

溶解度

动物实验配方

生物活性

描述NS1643 is a partial agonist of human ether-a-go-go-related gene (hERG) K(+) channels with an EC50 of 10.5 μM. NS1643 has distinct effects on erg2 (Kv11.2) currents by reducing channel inactivation especially at high concentrations^[3]. When assessed with 2-s depolarizations, NS1643 enhanced the magnitude of wild-type hERG (human ether-a-go-go-related gene) current in a concentration- and voltage-dependent manner with an EC(50) of 10.4 mM at -10 mV. NS1643 shifted the voltage dependence of inactivation by +21 mV at 10 mM and +35 mV at 30 mM, but it did not alter the voltage dependence of activation of hERG channels. The agonist activity of NS1643 was facilitated by mutations (F656 to Val, Met, or Thr) that are known to greatly attenuate channel inhibition by hERG blockers^[4].