| Bioactivity | E-4031 is a selective hERG potassium channel blocker for use in class III anti-arrhythmic studies[1]. |
| Invitro | E-4031 (0.1-10 μM) significantly depolarises the maximum diastolic potential (MDP) and prolongs the action charge that depolarises MDP from -58.8+0.9 to -24.5±1.8 mV at 1 μM and from -58.2±2.1 to -19.6±1.8 mV at 10 μM in single SAN cells of New Zealand albinc rabbits[2].E-4031 (0.1-10 μM) can block part of the outward current during the depolarisation step as well as the tail current (ITD) during subsequent repolarization in a dose-dependent manner, and depresses ITD by 88 % at 10 μM in single SAN cells of New Zealand albinc rabbits[2]. |
| In Vivo | E-4031 (i.v., 50 μg/kg) reduces the net outward current of ventricular myocytes, prolongs the QT interval and activation-recovery interval (ARI) in all left ventricular (LV) layers, and increases transmural ARI dispersion in beagles[1]. |
| Name | E-4031 |
| CAS | 113559-13-0 |
| Formula | C21H29Cl2N3O3S |
| Molar Mass | 474.44 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Daisuke Izumi, et al. Effects of bepridil versus E-4031 on transmural ventricular repolarization and inducibility of ventricular tachyarrhythmias in the dog. Pacing Clin Electrophysiol. 2010 Aug;33(8):950-9. [2]. E E Verheijck, et al. Effects of delayed rectifier current blockade by E-4031 on impulse generation in single sinoatrial nodal myocytes of the rabbit. Circ Res. 1995 Apr;76(4):607-15. |