| Identification | Back Directory | [Name]
N-[4-[[1-[2-(6-METHYL-2-PYRIDINYL)ETHYL]-4-PIPERIDINYL]CARBONYL]PHENYL]METHANESULFONAMIDE DIHYDROCHLORIDE | [CAS]
113558-89-7 | [Synonyms]
E-4031
E-4031 (free base)
E-4031 DIHYDROCHLORIDE
N-[4-[1-[2-(6-methylpyridin-2-yl)ethyl]piperidine-4-carbonyl]phenyl]methanesulfonamide
4'-[[1-[2-(6-METHYL-2-PYRIDINYL)ETHYL]-4-PIPERIDINYL]CARBONYL] METHANESULFONANILIDE, 2HCL
Methanesulfonamide, N-[4-[[1-[2-(6-methyl-2-pyridinyl)ethyl]-4-piperidinyl]carbonyl]phenyl]-
N-[4-[[1-[2-(6-METHYL-2-PYRIDINYL)ETHYL]-4-PIPERIDINYL]CARBONYL]PHENYL]METHANESULFONAMIDE DIHYDROCHLORIDE | [Molecular Formula]
C21H27N3O3S | [MDL Number]
MFCD01754739 | [MOL File]
113558-89-7.mol | [Molecular Weight]
401.52 |
| Chemical Properties | Back Directory | [Boiling point ]
561.7±60.0 °C(Predicted) | [density ]
1.243±0.06 g/cm3(Predicted) | [storage temp. ]
RT | [solubility ]
Soluble in DMSO (up to 25 mg/ml) or in Water (up to 100 mg/ml). | [form ]
White solid. | [pka]
7.11±0.10(Predicted) | [color ]
White | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 2 months. |
| Hazard Information | Back Directory | [Description]
E-4031 (113558-89-7) is a selective hERG potassium channel blocker. Inhibits the rapid delayed-rectifier K+ current (IKr). Class III antiarrhythmic agent. Cell permeable. | [Definition]
ChEBI: E-4031 is a sulfonamide. | [in vitro]
it has been reported that e-4031 could induce eads or tdp, and such induction correlated with a significant increase in variability of repolarization. in addition, e-4031 at 0.1 um was able to significantly prolong cycle length, action potential duration, and depolarized maximum diastolic potential. e-4031could also reduce the upstroke velocity of the action potential as well as the diastolic depolarization rate [1]. | [in vivo]
animal study showed that e-4031 at 0.01 and 0.1 mg/kg could provide effective in-vitro plasma concentrations to significantly inhibit ikr and thus delayed the repolarization beyond the initiation of diastole, leading to the inversion of electro-mechanical coupling, which provides an ideal proarrhythmic substrate [2]. another sutdy found that e-4031 could prolong qt interval and ari in all lv layers, though the magnitude of prolongation was greatest in mid, particularly during bradycardia [3]. | [IC 50]
7.7 nm for herg | [References]
1) Ficker et al. (2002), The binding site for channel blockers that rescue misprocessed human long QT syndrome type 2 ether-a-gogo gene (HERG) mutations; J. Biol. Chem., 277 4989
2) Wettwer et al. (1991), Effects of the new class III antiarrhythmic drug E-4031 on myocardial contractility and electrophysical parameters; J. Cardiovasc. Pharmacol., 17 480 |
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