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CAS No.: 448895-37-2

NS1643 Catalog No. CSN12824

Synonyms: NS-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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实验方案

技术信息

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].
参考文献

[1] Elmedyb P, Olesen SP, et al. Activation of ERG2 potassium channels by the diphenylurea NS1643. Neuropharmacology. 2007 Aug;53(2):283-94.
[2] Casis O, Olesen SP, et al. Mechanism of action of a novel human ether-a-go-go-related gene channel activator. Mol Pharmacol. 2006 Feb;69(2):658-65.
[3] Sun XJ, Man N, Tan Y, Nimer SD, Wang L. The Role of Histone Acetyltransferases in Normal and Malignant Hematopoiesis. Front Oncol. 2015;5:108.
[4] Casis O, Olesen SP, Sanguinetti MC. Mechanism of action of a novel human ether-a-go-go-related gene channel activator. Mol Pharmacol. 2006;69(2):658-665

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6299 mL
- 13.1495 mL
- 26.2990 mL
- 5 mM
- 0.5260 mL
- 2.6299 mL
- 5.2598 mL
- 10 mM
- 0.2630 mL
- 1.3150 mL
- 2.6299 mL

技术信息

CAS号

448895-37-2

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H10F6N2O3

运输

蓝冰

分子量

380.24

别名

NS-1643

溶解度

DMSO	76.0 mg/mL (199.9 mM)
Water	Insoluble
Ethanol	75.0 mg/mL (197.2 mM)

动物实验配方

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