N-[4-[[1-[2-(6-METHYL-2-PYRIDINYL)ETHYL]-4-PIPERIDINYL]CARBONYL]PHENYL]METHANESULFONAMIDE DIHYDROCHLORIDE
- Product Name
- N-[4-[[1-[2-(6-METHYL-2-PYRIDINYL)ETHYL]-4-PIPERIDINYL]CARBONYL]PHENYL]METHANESULFONAMIDE DIHYDROCHLORIDE
- CAS No.
- 113558-89-7
- Chemical Name
- N-[4-[[1-[2-(6-METHYL-2-PYRIDINYL)ETHYL]-4-PIPERIDINYL]CARBONYL]PHENYL]METHANESULFONAMIDE DIHYDROCHLORIDE
- 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
- CBNumber
- CB5749205
- Molecular Formula
- C21H27N3O3S
- Formula Weight
- 401.52
- MOL File
- 113558-89-7.mol
N-[4-[[1-[2-(6-METHYL-2-PYRIDINYL)ETHYL]-4-PIPERIDINYL]CARBONYL]PHENYL]METHANESULFONAMIDE DIHYDROCHLORIDE Property
- 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.
N-Bromosuccinimide Price
- Product number
- 324470
- Product name
- E-4031 - CAS 113558-89-7 - Calbiochem
- Purity
- A potent and selective inhibitor of the rapid type of inactivating inward-rectifying K+ current (IK, IR) (IC?? = 10 nM).
- Packaging
- 5MG
- Price
- $362
- Updated
- 2024/03/01
- Product number
- 1808
- Product name
- E-4031dihydrochloride
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $209
- Updated
- 2021/12/16
- Product number
- 1808
- Product name
- E-4031dihydrochloride
- Purity
- ≥98%(HPLC)
- Packaging
- 50
- Price
- $862
- Updated
- 2021/12/16
- Product number
- 255211
- Product name
- E-4031 dihydrochloride
- Packaging
- 10mg
- Price
- $466
- Updated
- 2021/12/16
- Product number
- API0015408
- Product name
- N-(4-(1-(2-(6-METHYLPYRIDIN-2-YL)ETHYL)PIPERIDINE-4-CARBONYL)PHENYL)METHANESULFONAMIDE
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $496.02
- Updated
- 2021/12/16
N-[4-[[1-[2-(6-METHYL-2-PYRIDINYL)ETHYL]-4-PIPERIDINYL]CARBONYL]PHENYL]METHANESULFONAMIDE DIHYDROCHLORIDE Chemical Properties,Usage,Production
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
N-[4-[[1-[2-(6-METHYL-2-PYRIDINYL)ETHYL]-4-PIPERIDINYL]CARBONYL]PHENYL]METHANESULFONAMIDE DIHYDROCHLORIDE Preparation Products And Raw materials
Raw materials
Preparation Products
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