E-4031 dihydrochloride

Name: E-4031 dihydrochloride
Brand: Tocris Bioscience
SKU: 1808
Rating: 5 (2 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 1808

(2)

Citations (18)

COA / SDS

KV11.1 (hERG) channel blocker; inhibits rapid delayed rectifier K+ current (IKr)

Key Product Details

Description:	K_V11.1 (hERG) channel blocker; inhibits rapid delayed rectifier K⁺ current (I_Kr)
Chemical Name:	N-[4-[[1-[2-(6-Methyl-2-pyridinyl)ethyl]-4-piperidinyl]carbonyl]phenyl]methanesulfonamide dihydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	474.44

View Full Technical Details for E-4031 dihydrochloride

Technical Data
Citations / Reviews (2)

Biological Activity for E-4031 dihydrochloride

E-4031 dihydrochloride is a selective blocker of K_V11.1 (hERG) channels; inhibits the rapid delayed-rectifier K⁺ current (I_Kr). 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 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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References for E-4031 dihydrochloride

References are publications that support the biological activity of the product.

Verheijck Effects of the delayed rectifier current blockade by E-4031 on impulse generation in single sinoatrial nodal myocytes of the rabbit. Circ.Res. 1995 PMID: 7895335
Wettwer Effects of the new class III antiarrhythmic drug E-4031 on myocardial contractility and electrophysiological parameters. J.Cardiovasc.Pharmacol. 1991 PMID: 1711611
Ficker 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. 2002 PMID: 11741928