NS3623

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Chemical Structure| 343630-41-1 同义名 : -
CAS号 : 343630-41-1
货号 : A1209642
分子式 : C15H10BrF3N6O
纯度 : 99%+
分子量 : 427.18
MDL号 : MFCD22683830
存储条件：

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

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
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].
实验方案
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
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.