E-4031 dihydrochloride

Pricing Availability Delivery Time Qty
Cat.No. 1808 - E-4031 dihydrochloride | C21H27N3O3S.2HCl | CAS No. 113559-13-0
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)
Datasheet
Citations (4)
Literature

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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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


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View Related Products by Product Action

View all Voltage-gated Potassium (KV) Channel Blockers

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

4 Citations for E-4031 dihydrochloride

Citations are publications that use Tocris products. Selected citations for E-4031 dihydrochloride include:

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

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

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


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