N-[4-[[1-[2-(6-METHYL-2-PYRIDINYL)ETHYL]-4-PIPERIDINYL]CARBONYL]PHENYL]METHANESULFONAMIDE DIHYDROCHLORIDE
Synonym(s):4ʹ-[[1-[2-(6-Methyl-2-pyridinyl)ethyl-4-piperidinyl]carbonyl]methanesulfonanilide, 2HCl;E-4031 - CAS 113558-89-7 - Calbiochem
- CAS NO.:113558-89-7
- Empirical Formula: C21H27N3O3S
- Molecular Weight: 401.52
- MDL number: MFCD01754739
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-05-18 11:31:09
What is N-[4-[[1-[2-(6-METHYL-2-PYRIDINYL)ETHYL]-4-PIPERIDINYL]CARBONYL]PHENYL]METHANESULFONAMIDE DIHYDROCHLORIDE?
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].
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
Properties of N-[4-[[1-[2-(6-METHYL-2-PYRIDINYL)ETHYL]-4-PIPERIDINYL]CARBONYL]PHENYL]METHANESULFONAMIDE DIHYDROCHLORIDE
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). |
pka | 7.11±0.10(Predicted) |
form | White solid. |
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. |
Safety information for N-[4-[[1-[2-(6-METHYL-2-PYRIDINYL)ETHYL]-4-PIPERIDINYL]CARBONYL]PHENYL]METHANESULFONAMIDE DIHYDROCHLORIDE
Computed Descriptors for N-[4-[[1-[2-(6-METHYL-2-PYRIDINYL)ETHYL]-4-PIPERIDINYL]CARBONYL]PHENYL]METHANESULFONAMIDE DIHYDROCHLORIDE
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