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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Company Name: |
MedBioPharmaceutical Technology Inc
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Tel: |
021-69568360 18916172912 |
Email: |
order@med-bio.cn |
Products Intro: |
Product Name:N-[4-[[1-[2-(6-METHYL-2-PYRIDINYL)ETHYL]-4-PIPERIDINYL]CARBONYL]PHENYL]METHANESULFONAMIDE DIHYDROCHLORIDE CAS:113558-89-7 Purity:98% Package:10mg; 50mg; 5mg Remarks:Medbio
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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. | 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 |
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