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Submit ReviewE-4031 dihydrochloride
Description: KV11.1 (hERG) channel blocker; inhibits rapid delayed rectifier K+ current (IKr)
Chemical Name: N-[4-[[1-[2-(6-Methyl-2-pyridinyl)ethyl]-4-piperidinyl]carbonyl]phenyl]methanesulfonamide dihydrochloride
Purity: ≥98% (HPLC)
Biological Activity 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.
Compound Libraries for E-4031 dihydrochloride
E-4031 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for E-4031 dihydrochloride
| M. Wt | 474.44 |
| Formula | C21H27N3O3S.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for E-4031 dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 47.44 | 100 | |
| DMSO | 9.49 | 20 with gentle warming |
Preparing Stock Solutions for E-4031 dihydrochloride
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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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Product Datasheets for E-4031 dihydrochloride
References for E-4031 dihydrochloride
References are publications that support the biological activity of the product.
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.
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Keywords: 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 Citations for E-4031 dihydrochloride
Citations are publications that use Tocris products. Selected citations for E-4031 dihydrochloride include:
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
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
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
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
Fiore et al (2013) Characterization of hERG1 channel role in mouse colorectal carcinogenesis. Cancer Med 2 583 PMID: 24403225
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
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
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
Do you know of a great paper that uses E-4031 dihydrochloride from Tocris? Please let us know.
Reviews for E-4031 dihydrochloride
Average Rating: 5 (Based on 2 Reviews.)
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E-4031 shortens cardiac action potential duration.
By
Anonymous on 05/16/2019
Assay Type: In Vitro
Species: Other
Cell Line/Tissue: 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
Assay Type: In Vitro
Species: 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.
