| Company Name: |
3B Pharmachem (Wuhan) International Co.,Ltd.
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| Tel: |
821-50328103-801 18930552037 |
| Email: |
3bsc@sina.com |
| Products Intro: |
Product Name:N-[4-[[1-[2-(6-METHYL-2-PYRIDINYL)ETHYL]-4-PIPERIDINYL]CARBONYL]PHENYL]METHANESULFONAMIDE DIHYDROCHLORIDE
CAS:113558-89-7
Purity:99% HPLC Package:1Mg ; 5Mg;10Mg ;100Mg;250Mg ;500Mg ;1g;2.5g ;5g ;10g
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Email: |
eric_feng1954@126.com |
| Products Intro: |
Product Name:E-4031 (free base)
CAS:113558-89-7
Purity:95% -98%HPLC Package:1GR;10GR;50GR;100GR;250GR;500GR;1KG;5KG;10KG;100KG
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| | N-[4-[[1-[2-(6-METHYL-2-PYRIDINYL)ETHYL]-4-PIPERIDINYL]CARBONYL]PHENYL]METHANESULFONAMIDE DIHYDROCHLORIDE Basic information |
| | N-[4-[[1-[2-(6-METHYL-2-PYRIDINYL)ETHYL]-4-PIPERIDINYL]CARBONYL]PHENYL]METHANESULFONAMIDE DIHYDROCHLORIDE Chemical Properties |
| 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-[4-[[1-[2-(6-METHYL-2-PYRIDINYL)ETHYL]-4-PIPERIDINYL]CARBONYL]PHENYL]METHANESULFONAMIDE DIHYDROCHLORIDE Usage And Synthesis |
| 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. | | Uses | E-4031 free base is a selective hERG potassium channel blocker for use in class III anti-arrhythmic studies[1]. | | 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] E. FICKER. The Binding Site for Channel Blockers That Rescue Misprocessed Human Long QT Syndrome Type 2 ether-a-gogo-related Gene (HERG) Mutations*[J]. The Journal of Biological Chemistry, 2002, 122 1: 4989-4998. DOI:10.1074/jbc.m107345200
[2] E WETTWER. Effects of the new class III antiarrhythmic drug E-4031 on myocardial contractility and electrophysiological parameters.[J]. Journal of Cardiovascular Pharmacology, 1991, 17 3: 480-487. DOI:10.1097/00005344-199103000-00018 |
| | N-[4-[[1-[2-(6-METHYL-2-PYRIDINYL)ETHYL]-4-PIPERIDINYL]CARBONYL]PHENYL]METHANESULFONAMIDE DIHYDROCHLORIDE Preparation Products And Raw materials |
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