产品说明书

NS1643

Print
Chemical Structure| 448895-37-2 同义名 : -
CAS号 : 448895-37-2
货号 : A355887
分子式 : C15H10F6N2O3
纯度 : 99%+
分子量 : 380.242
MDL号 : MFCD08705418
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(276.14 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.63mL

0.53mL

0.26mL

13.15mL

2.63mL

1.31mL

26.30mL

5.26mL

2.63mL
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