Biological Activity
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
E-4031 dihydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 23.72 | 50 | |
| water | 47.44 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 474.44. Batch specific molecular weights may vary from batch to batch due to solvent 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
References
References are publications that support the products' biological activity.
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
Keywords: 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, Potassium, Channels, Voltage-Gated, Potassium, Channels, Tocris Bioscience
