NS3623 是hERG1 (KV11.1)钾通道激活剂，激活IKr和Ito电流，具有抗心律失常作用。NS3623也是 hERG1 通道抑制剂。

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.

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 [3].

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 [1].

343630-41-1

C15H10BrF3N6O

427.18

NS3623

DMSO:9.17 mg/ml (21.46 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years