E-4031
E-4031 structure
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Common Name | E-4031 | ||
|---|---|---|---|---|
| CAS Number | 113559-13-0 | Molecular Weight | 474.444 | |
| Density | N/A | Boiling Point | 561.7ºC at 760 mmHg | |
| Molecular Formula | C21H29Cl2N3O3S | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | 293.5ºC | |
Use of E-4031E-4031 is a benzenesulfonamide antiarrhythmic agent; blocks the ATP-sensitive potassium channel.IC50 value:Target: K+ channel blockerin vitro: Dofetilide and E-4031 induced EADs or TdP in all assays (50-83%), and the induction correlated with a significant increase in beat-to-beat variability of repolarization [1]. E-4031 (0.1 mumol/L) significantly prolonged cycle length and action potential duration, depolarized maximum diastolic potential, and reduced both the upstroke velocity of the action potential and the diastolic depolarization rate [2].in vivo: E-4031 in doses of 0.01 and 0.1 mg/kg that can provide the plasma concentrations effectively to inhibit IKrin vitro significantly delayed the repolarization beyond the initiation of diastole, resulting in the inversion of electro-mechanical coupling, which provides an ideal proarrhythmic substrate, while the durations of left ventricular systole and diastole remained the same [3]. Bepridil and E-4031 prolonged QT interval and ARI in all LV layers, though the magnitude of prolongation was greatest in Mid, increasing the transmural ARI dispersion, particularly during bradycardia [4]. |
| Name | N-[4-[1-[2-(6-methylpyridin-2-yl)ethyl]piperidine-4-carbonyl]phenyl]methanesulfonamide,dihydrochloride |
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| Synonym | More Synonyms |
| Description | E-4031 is a benzenesulfonamide antiarrhythmic agent; blocks the ATP-sensitive potassium channel.IC50 value:Target: K+ channel blockerin vitro: Dofetilide and E-4031 induced EADs or TdP in all assays (50-83%), and the induction correlated with a significant increase in beat-to-beat variability of repolarization [1]. E-4031 (0.1 mumol/L) significantly prolonged cycle length and action potential duration, depolarized maximum diastolic potential, and reduced both the upstroke velocity of the action potential and the diastolic depolarization rate [2].in vivo: E-4031 in doses of 0.01 and 0.1 mg/kg that can provide the plasma concentrations effectively to inhibit IKrin vitro significantly delayed the repolarization beyond the initiation of diastole, resulting in the inversion of electro-mechanical coupling, which provides an ideal proarrhythmic substrate, while the durations of left ventricular systole and diastole remained the same [3]. Bepridil and E-4031 prolonged QT interval and ARI in all LV layers, though the magnitude of prolongation was greatest in Mid, increasing the transmural ARI dispersion, particularly during bradycardia [4]. |
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| Related Catalog | |
| References |
| Boiling Point | 561.7ºC at 760 mmHg |
|---|---|
| Molecular Formula | C21H29Cl2N3O3S |
| Molecular Weight | 474.444 |
| Flash Point | 293.5ºC |
| Exact Mass | 473.130676 |
| PSA | 87.75000 |
| LogP | 5.59460 |
| Vapour Pressure | 1.21E-12mmHg at 25°C |
| Storage condition | 2-8℃ |
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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| RIDADR | NONH for all modes of transport |
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| Methanesulfonamide, N-[4-[[1-[2-(6-methyl-2-pyridinyl)ethyl]-4-piperidinyl]carbonyl]phenyl]-, hydrochloride (1:2) |
| N-[4-({1-[2-(6-Methyl-2-pyridinyl)ethyl]-4-piperidinyl}carbonyl)phenyl]methanesulfonamide dihydrochloride |
| E-4031 |
| N-(4-(1-(2-(6-methylpyridin-2-yl)ethyl)piperidine-4-carbonyl)phenyl)methanesulfonamide dihydrochloride |
| N-[4-({1-[2-(6-Methylpyridin-2-yl)ethyl]piperidin-4-yl}carbonyl)phenyl]methanesulfonamide dihydrochloride |
| MFCD01754739 |
| E 4031 dihydrochloride |
| PDZ1 Domain inhibitor peptide |