Biological descriptionType III antiarrhythmic drug that blocks ion channels encoded by the ether-a-go-go related gene (ERG1 or KCNH1). Blocks channels in the open configuration with little effect on the channels in the closed configuration. The IC50 for block of human ERG channels in expression systems is approx. 350 nM.
Chemical nameN-[4-[[1-[2-(6-Methyl-2-pyridinyl)ethyl]-4-piperidinyl]carbonyl]phenyl]methanesulfonamide dihydrochloride
Storage instructionsStore at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months.
Solubility overviewSoluble in water to 100 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Herzberg IM et al. Transfer of rapid inactivation and sensitivity to the class III antiarrhythmic drug E-4031 from HERG to M-eag channels. J Physiol511 ( Pt 1):3-14 (1998).
Read more (PubMed: 9679158) »
Spector PS et al. Class III antiarrhythmic drugs block HERG, a human cardiac delayed rectifier K+ channel. Open-channel block by methanesulfonanilides. Circ Res78:499-503 (1996).
Read more (PubMed: 8593709) »
Sanguinetti MC & Jurkiewicz NK Two components of cardiac delayed rectifier K+ current. Differential sensitivity to block by class III antiarrhythmic agents. J Gen Physiol96:195-215 (1990).
Read more (PubMed: 2170562) »