Biochem/physiol Actions

Cell permeable: no

Reversible: no

Target IC₅₀: 10 nM inhibiting the rapid type of inactivating inward-rectifying K+ current

Product does not compete with ATP.

Primary TargetInhibitor of the rapid type of inactivating inward-rectifying K+ current

General description

A potent and selective inhibitor of the rapid type of inactivating inward-rectifying K⁺ current (IK, IR) (IC₅₀ = 10 nM). A class III anti-arrhythmic agent with differential atrial versus ventricular activity. A specific blocker of HERG channels (IC₅₀ = 7.7 nM).

A potent and selective inhibitor of the inactivating inward-rectifying potassium current (IK,IR) (IC₅₀ = 10 nM). In inside-out patches, E-4031 also blocks ATP sensitive K⁺ channel (EC₅₀ = 31 µM). A specific blocker of cardiac HERG channels (IC₅₀ = 7.7 nM). A class III anti-arrhythmic agent with differential atrial versus ventricular activity.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Ficker, E., et al. 2000. Am. J. Physiol.279, H1748.Ono, K., et al. 2000. J. Physiol. (London)524 (Pt. 1), 51.Xie, J.T., et al. 2000. Methods Find. Exp. Clin. Pharmacol.22, 67.Bauer, C.K., et al. 1999. Mol. Cell Endocrinol. 148, 37.Baskin, E.P., and Lynch, J.J. 1998. J. Pharmacol. Exp. Ther. 285, 135.Weinsberg, F., et al. 1997. Pflugers Arch. 434, 1.West, P.D., et al. 1997. J. Cardiovasc. Pharmacol. Ther.2, 205.West, P.D., et al. 1996. Pharmacol. Toxicol.78, 89.

Packaging

5 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)