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NS3623 {[allProObj[0].p_purity_real_show]}

货号:A1209642

NS3623 is an activator of both hERG and Kv4.3.

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NS3623 化学结构 CAS号:343630-41-1
NS3623 化学结构
CAS号:343630-41-1
NS3623 3D分子结构
CAS号:343630-41-1
NS3623 化学结构 CAS号:343630-41-1
NS3623 3D分子结构 CAS号:343630-41-1
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NS3623 纯度/质量文件 产品仅供科研

货号:A1209642 标准纯度: {[allProObj[0].p_purity_real_show]}
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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。

NS3623 生物活性

描述 The human ether-à-go-go related gene (HERG) encodes the alpha subunit of Kv11.1, which is a voltage-gated K+ channel protein mainly expressed in heart and brain tissue. HERG plays critical role in cardiac repolarization, and mutations in HERG can cause long QT syndrome[1]. NS3623 is an activator of human ether-a-go-go-related gene potassium channels. NS3623 has a dual mode of action, being an inhibitor of hERG1 channels. NS3623 activates the IKr and Ito currents and has an antiarrhythmic effect[2]. NS3623 (30 mg/kg; i.v.; lasting for 3 minutes) shortens the corrected QT interval by 25 +/- 4% in anaesthetized guinea pigs. NS3623 (50 mg/kg) immediately reduces the QTcF interval and remains obviously shortened for approximately 30 minutes. NS3623 (50 mg/kg) shortens the QT interval by 30 +/- 6% in conscious guinea pigs[3]. The application of NS3623 (5 μM) greatly increases the size of the tail current confirming previous studies demonstrating this drug increased IKr, in isolated canine cardiomyocytes. NS3623 enhances IKr tail currents (at +50 mV activating pulse) by 60% in normal Mid cells, and 68% in 48 h cultured cells. The effect of NS3623 on IKr recorded from cells kept in culture is evaluated. The magnitude of IKr is greatly decreased compared to freshly isolated cells, after 48 h. Peak IKr tail currents are 0.47 ± 0.08 pA/pF in freshly isolated myocytes and 0.28 ± 0.06 pA/pF in 2-day cultured myocytes. Application of NS3623 increases IKr in cultured Mid cells. Analysis of the current-voltage (I-V) relation of IKr tail current showed that NS3623 increased current density in both 1 day and 2-day cultured Mid cells[4].

NS3623 参考文献

[1]Siyi He,et al. HERG channel and cancer: A mechanistic review of carcinogenic processes and therapeutic potential. Biochim Biophys Acta Rev Cancer.2020 Apr;1873(2):188355.

[2]Diness JG, et al. Antiarrhythmic effect of IKr activation in a cellular model of LQT3. Heart Rhythm. 2009 Jan;6(1):100-6.

[3] Hansen RS, et al. In vivo effects of the IKr agonist NS3623 on cardiac electrophysiology of the guinea pig. J Cardiovasc Pharmacol. 2008 Jul;52(1):35-41.

[4]Calloe K, et al. A dual potassium channel activator improves repolarization reserve and normalizes ventricular action potentials. Biochem Pharmacol. 2016 May 15;108:36-46.

NS3623 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.34mL

0.47mL

0.23mL

11.70mL

2.34mL

1.17mL

23.41mL

4.68mL

2.34mL

NS3623 技术信息

CAS号343630-41-1
分子式C15H10BrF3N6O
分子量 427.18
SMILES Code O=C(NC1=CC=CC(C(F)(F)F)=C1)NC2=CC=C(Br)C=C2C3=NN=NN3
MDL No. MFCD22683830
别名
运输蓝冰
InChI Key JXPULDIATMTIIN-UHFFFAOYSA-N
Pubchem ID 9954236
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
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