E-4031 is a methanesulfonanilide class III antiarrhythmic agent known to inhibit KV11.1 (hERG) channels. Sub-micromolar concentration of E-4031, selectively blocks Kv11.1 channels, either in heterologous systems,cardiac cells and cardiac preparations. E-4031 was shown to rescue the functional expression of mutated (LQ2) KV11.1 channels in HEK cells. E-4031 (40 µM) treatment also prevented FAK phosphorylation and Rac1 activity (only in HEK cells expressing the KV11.1 subunit). In rat carotid chemoreceptor cells, 1 µM E-4031 inhibited the KV current, to a larger extent in postnatal cells, establishing the developmental disappearance of KV11.1 channels and their contribution to the response to hypoxia. E-4031 (1 µM) accelerated myoblast fusion, probably by blocking KV11.1 channels that leads to depolarization.
产品描述
A Blocker of KV11.1 (hERG) K+ Channels
产品形式
E-4031 is a methanesulfonanilide class III antiarrhythmic agent known to inhibit KV11.1 (hERG) channels. Sub-micromolar concentration of E-4031, selectively blocks Kv11.1 channels, either in heterologous systems,cardiac cells and cardiac preparations. E-4031 was shown to rescue the functional expression of mutated (LQ2) KV11.1 channels in HEK cells. E-4031 (40 µM) treatment also prevented FAK phosphorylation and Rac1 activity (only in HEK cells expressing the KV11.1 subunit). In rat carotid chemoreceptor cells, 1 µM E-4031 inhibited the KV current, to a larger extent in postnatal cells, establishing the developmental disappearance of KV11.1 channels and their contribution to the response to hypoxia. E-4031 (1 µM) accelerated myoblast fusion, probably by blocking KV11.1 channels that leads to depolarization.