Uses
E-4031 has been used as:
- human ether-a-go-go-related gene (hERG) blocker in human-induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs)
- IKr blocker in long QT syndrome (LQTS) induced pluripotent stem (iPSCs) embryoid bodies
- IKr blocker in rat ventricular myocytes
Biological Activity
Selective blocker of hERG K + channels; inhibits the rapid delayed-rectifier K + current (I Kr ). Reversibly prolongs action potential duration in guinea pig papillary muscle and isolated ventricular myocytes, without affecting Na + or Ca 2+ inward currents. Class III antiarrhythmic agent.
Biochem/physiol Actions
E-4031 is a antiarrhythmic drug and belongs to the class III type. It is a methanesulfonanilide compound and is effective in treating arrhythmia and modulates ventricular fibrillation. E-4031 mediates the prolongation of action potential duration (APD) in transgenic long-QT type 1 (LQT1) rabbits. An isoleucine mutation in human ether-a-go-go-related gene (hERG) abolishes its interaction with E-4031.
storage
Room temperature (desiccate)
