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NS1643 {[allProObj[0].p_purity_real_show]}

货号:A355887

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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NS1643 化学结构 CAS号:448895-37-2
NS1643 化学结构
CAS号:448895-37-2
NS1643 3D分子结构
CAS号:448895-37-2
NS1643 化学结构 CAS号:448895-37-2
NS1643 3D分子结构 CAS号:448895-37-2
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NS1643 纯度/质量文件 产品仅供科研

货号:A355887 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Potassium Channel 其他靶点 纯度
Tolbutamide 98%
Glimepiride ++++

SUR1, IC50: 5.4 nM

SUR2B, IC50: 7.3 nM

97%
Dronedarone Hydrochloride 95%
Gliquidone ++

Potassium channel, IC50: 27.2 nM

98%
TRAM-34 +++

IKCa1 (KCa3.1), Kd: 20 nM

98%
Glibenclamide 98%
Amiodarone HCl 97%
Gliclazide ++

Potassium channel, IC50: 184 nM

98%
Repaglinide 98%
Dofetilide 98%
Nateglinide 99%
Quinine hydrochloride dihydrate 98%
ML133 HCl +

Kir2.1, IC50: 290 nM

97%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

NS1643 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].

NS1643 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

NS1643 实验方案

计算器
存储液制备 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

NS1643 技术信息

CAS号448895-37-2
分子式C15H10F6N2O3
分子量 380.242
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

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

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