NS-1643 is a potent and selective KV11.1 channel modulator (enhancer). In Xenopus oocytes and in HEK-293 cells, NS-1643 increased both steady-state and tail current at all voltages. The EC50 value for hERG channel activation was 10.5 µM – 20 µM. In guinea pig cardiomyocytes, application of 10 µM NS-1643 activated IKr and significantly decreased the action potential duration to 65% of the control values. Accordingly, NS-1643 reversed acquired LQTS and Torsades de Pointes (TdP) in rabbits, caused by bradycardic remodelling and hERG-blocking drugs.
产品描述
An Opener of KV11.1 and KCNQ K+ Channels
产品形式
The KV11.1 (hERG, ERG1, erg1) channel is a member of the ether-a-go-go (EAG) subfamily of voltage-dependent K+ channels that includes the related proteins KV11.2 and KV11.3 (erg2 and erg3). The KV11.1 current is characterized by strong inward rectification with slow activation and very rapid inactivation kinetics. The channel is expressed in the brain and heart (where it underlies the IKr current) and has a central role in mediating repolarization of action potentials.
