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Submit ReviewE-4031 dihydrochloride
说明： KV11.1 (hERG) channel blocker; inhibits rapid delayed rectifier K+ current (IKr)
化学名： N-[4-[[1-[2-(6-Methyl-2-pyridinyl)ethyl]-4-piperidinyl]carbonyl]phenyl]methanesulfonamide dihydrochloride
纯度： ≥98% (HPLC)
生物活性 for E-4031 dihydrochloride
E-4031 dihydrochloride is a selective blocker of KV11.1 (hERG) channels; inhibits the rapid delayed-rectifier K+ current (IKr). Reversibly prolongs action potential duration in guinea pig papillary muscle and isolated ventricular myocytes, without affecting Na+ or Ca2+ inward currents. Class III antiarrhythmic agent.
化合物库 for E-4031 dihydrochloride
E-4031 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for E-4031 dihydrochloride
| 分子量 | 474.44 |
| 公式 | C21H27N3O3S.2HCl |
| 储存 | Desiccate at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 113559-13-0 |
| PubChem ID | 3087190 |
| InChI Key | ZQBNWMFBOSOOLX-UHFFFAOYSA-N |
| Smiles | Cl.Cl.CC1=CC=CC(CCN2CCC(CC2)C(=O)C2=CC=C(NS(C)(=O)=O)C=C2)=N1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for E-4031 dihydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 47.44 | 100 | |
| DMSO | 9.49 | 20 温和加热 |
制备储备液 for E-4031 dihydrochloride
以下数据基于产品分子量 474.44。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.11 mL | 10.54 mL | 21.08 mL |
| 5 mM | 0.42 mL | 2.11 mL | 4.22 mL |
| 10 mM | 0.21 mL | 1.05 mL | 2.11 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
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产品说明书 for E-4031 dihydrochloride
参考文献 for E-4031 dihydrochloride
参考文献是支持产品生物活性的出版物。
Ficker et al (2002) The binding site for channel blockers that rescue misprocessed human long QT syndrome type 2 ether-a-gogo-related gene (HERG) mutations. J.Biol.Chem. 277 4989 PMID: 11741928
Verheijck et al (1995) Effects of the delayed rectifier current blockade by E-4031 on impulse generation in single sinoatrial nodal myocytes of the rabbit. Circ.Res. 76 607 PMID: 7895335
Wettwer et al (1991) Effects of the new class III antiarrhythmic drug E-4031 on myocardial contractility and electrophysiological parameters. J.Cardiovasc.Pharmacol. 17 480 PMID: 1711611
If you know of a relevant reference for E-4031 dihydrochloride, please let us know.
关键词: E-4031 dihydrochloride, E-4031 dihydrochloride supplier, HERG, KV11.1, channel, blockers, inhibits, inhibitors, rapid, delayed, rectifier, K+, current, IKr, Potassium, KV, Channels, Human, Ether-A-Go-Go, Gene, voltage-gated, voltage-dependent, Voltage-Gated, 1808, Tocris Bioscience
11 篇 E-4031 dihydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 E-4031 dihydrochloride 的部分引用包括：
Zhang et al (2017) Differentiation and characterization of rhesus monkey atrial and ventricular cardiomyocytes from induced pluripotent stem cells. Stem Cell Res 20 21 PMID: 28249229
Pei et al (2017) Chemical-defined and albumin-free generation of human atrial and ventricular myocytes from human pluripotent stem cells. Stem Cell Res 19 94 PMID: 28110125
Bragança et al (2016) Ion Fluxes through KCa2 (SK) and Cav1 (L-type) Channels Contribute to Chronoselectivity of Adenosine A1 Receptor-Mediated Actions in Spontaneously Beating Rat Atria. Front Pharmacol 7 45 PMID: 27014060
Zhang et al (2015) Cardiac sodium/calcium exchanger preconditioning promotes anti-arrhythmic and cardioprotective effects through mitochondrial calcium-activated potassium channel. PLoS One 8 10239 PMID: 26617732
Song et al (2022) Sigma non-opioid receptor 1 is a potential therapeutic target for long QT syndrome. Nat.Card.Res. 1 142 PMID: 36051854
Veldkamp et al (2018) Neurokinin-3 receptor activation selectively prolongs atrial refractoriness by inhibition of a background K+ channel. Nat Commun 9 4357 PMID: 30341287
Kamiya et al (2018) Electrophysiological measurement of ion channels on plasma/organelle membranes using an on-chip lipid bilayer system. Sci Rep 8 17498 PMID: 30504856
McKeithan et al (2017) An Automated Platform for Assessment of Congenital and Drug-Induced Arrhythmia with hiPSC-Derived Cardiomyocytes. Front Physiol 8 766 PMID: 29075196
Guo et al (2015) Use of Human Induced Pluripotent Stem Cell-Derived Cardiomyocytes (hiPSC-CMs) to Monitor Compound Effects on Cardiac Myocyte Signaling Pathways. Curr Protoc Chem Biol 7 141 PMID: 26331525
Yu et al (2014) Apamin does not inhibit human cardiac Na+ current, L-type Ca2+ current or other major K+ currents. Int J Clin Exp Pathol 9 e96691 PMID: 24798465
Fiore et al (2013) Characterization of hERG1 channel role in mouse colorectal carcinogenesis. Cancer Med 2 583 PMID: 24403225
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E-4031 dihydrochloride 的评论
平均评分: 5 (基于 2 条评论。)
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E-4031 shortens cardiac action potential duration.
By
Anonymous on 05/16/2019
分析类型： In Vitro
种属： Other
细胞系/组织： Cardiomyocytes
A representative action potential of a guinea pig cardiomyocyte before and after perfusion with 500 nM E-4031 for 5 min and stimulated at a frequency of 1 Hz in a whole cell patch clamp model. E-4031 significantly shortened action potential duration of guinea pig ventricular cardiomyocytes.
Antiarrhythmic drug E-4031 was studied to identify drug effect: Overall great product.
By
Anonymous on 10/22/2018
分析类型： In Vitro
种属： Human
As an antiarrhythmic drug E-4031 was studied to identify drug effect. Concentration dependent Kv channel blocking and control of release were studied. The compound showed blocking activity which is not dependent on concentration administered and data was reproducible. Great product stability and dissolves nicely.
