NS3623_product_DataBase

Bioactivity

NS3623 is an activator of human ether-a-go-go-related gene (hERG1/KV11.1) potassium channels. NS3623 activates the IKr and Ito currents and has antiarrhythmic effect. NS3623 has a dual mode of action, being an inhibitor of hERG1 channels[1][2][3].

Invitro

在分离的犬心肌细胞中，NS3623 (5 μM) 的应用大大增加了尾流的大小，证实了先前的研究表明该药物增加了 IKr。NS3623 对培养细胞IKr的影响也进行了评估。48 小时后，与新分离的细胞相比，IKr 的大小大大降低。新分离心肌细胞IKr 尾流峰值为0.47±0.08 pA/pF，培养2天的心肌细胞IKr 尾流峰值为 0.28±0.06 pA/pF。NS3623 的应用增加了培养的中间细胞的 IKr。对 IKr 尾流的电流电压 (I-V) 关系的分析表明，NS3623 在培养 1 天和 2 天的

In Vivo

在麻醉豚鼠中，NS3623 (30mg/kg；静脉注射；持续 3 分钟) 使校正的QT间期缩短 25±4%[1]。在清醒豚鼠中，NS3623 (50 mg/kg) 使QT间期缩短 30±6%。NS3623 (50 mg/kg) 立即缩短 QTcF 间隔，并显著缩短约 30 分钟[1]。 Animal Model:

Name

NS3623

CAS

343630-41-1

Formula

C15H10BrF3N6O

Molar Mass

427.18

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. 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. [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]. 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. [4]. Hansen RS, et al. Biophysical characterization of the new human ether-a-go-go-related gene channel opener NS3623 [N-(4-bromo-2-(1H-tetrazol-5-yl)-phenyl)-N'-(3'-trifluoromethylphenyl)urea]. Mol Pharmacol. 2006 Oct;70(4):1319-29.

PeptideDB

NS3623

CAS: 343630-41-1 F: C15H10BrF3N6O W: 427.18