An antiarrhythmic, ERG potassium channel blocker
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E-4031 (hydrochloride)

Item No. 15203

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[[1-[2-(6-methyl-2-pyridinyl)ethyl]-4-piperidinyl]carbonyl]phenyl]-methanesulfonamide, dihydrochloride
CAS Number
113559-13-0
Molecular Formula
C21H27N3O3S • 2HCl
Formula Weight
474.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 0.3 mg/mlDMSO: 25 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
273 nm
SMILES
O=C(C1CCN(CCC2=CC=CC(C)=N2)CC1)C3=CC=C(NS(C)(=O)=O)C=C3.Cl.Cl
InChi Code
InChI=1S/C21H27N3O3S.2ClH/c1-16-4-3-5-19(22-16)12-15-24-13-10-18(11-14-24)21(25)17-6-8-20(9-7-17)23-28(2,26)27;;/h3-9,18,23H,10-15H2,1-2H3;2*1H
InChi Key
ZQBNWMFBOSOOLX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $90

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    10 mg

    $158

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    25 mg

    $370

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    50 mg

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    Product Description

    E-4031 is a methanesulfonanilide class III antiarrhythmic agent that prolongs cardiac action potential duration by blocking ERG K+ channels (IC50 = 29 nM).1,2 E-4031 inhibits the ERG1, ERG2, and ERG3 isoforms with KD values of 99, 116, and 193 nM, respectively.3 However, at higher μM concentrations E-4031 can demonstrate pro-arrhythmic activity, inducing early after depolarizations (prolonged repolarization) in cell models and torsade de pointes in animal models.4 E-4031 has been used to pharmacologically rescue misprocessed ERG in long QT syndrome type 2, an autosomal dominant cardiac disease associated with prolongation of the QT interval and torsade de pointes.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jurkiewicz, N.K., and Sanguinetti, M.C. Rate-dependent prolongation of cardiac action potentials by a methanesulfonanilide class III antiarrhythmic agent. Circ. Res. 72(1), 75-83 (1993).

    2. Du, L.P., Tsai, K.C., Li, M.Y., et al. The pharmacophore hypotheses of IKr potassium channel blockers: Novel class III antiarrhythmic agents. Bioorg. Med. Chem. Lett. 14(18), 4771-4777 (2004).

    3. Shi, W., Wymore, R.S., Wang, H.S., et al. Identification of two nervous system-specific members of the erg potassium channel gene family. J. Neurosci. 17(24), 9423-9432 (1997).

    4. Nalos, L., Varkevisser, R., Jonsson, M.K., et al. Comparison of the IKr blockers moxifloxacin, dofetilide and E-4031 in five screening models of pro-arrhythmia reveals lack of specificity of isolated cardiomyocytes. Br. J. Pharmacol. 165(2), 467-478 (2012).

    5. Ficker, E., Obejero-Paz, C.A., Zhao, S., et al. The binding site for channel blockers that rescue misprocessed human long QT syndrome type 2 ether-a-gogo-related gene (HERG) mutations. The Journal of Biological Chemisty 277(7), 4989-4998 (2002).