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E-4031

Name: E-4031
Brand: MM

≥98% (HPLC), solid, K⁺ current inhibitor, Calbiochem^®

Synonym(s):

E-4031, 4ʹ-[[1-[2-(6-Methyl-2-pyridinyl)ethyl-4-piperidinyl]carbonyl]methanesulfonanilide, 2HCl

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About This Item

Empirical Formula (Hill Notation):

C₂₁H₂₇N₃O₃S · 2HCl · 2H₂O

CAS Number:

113558-89-7

Molecular Weight:

510.47

MDL number:

MFCD07363980

UNSPSC Code:

12352200

NACRES:

NA.77

Assay:

≥98% (HPLC)

Form:

solid

Quality level:

100

Storage condition:

OK to freeze, desiccated (hygroscopic)

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Properties

Product Name

E-4031, A potent and selective inhibitor of the rapid type of inactivating inward-rectifying K⁺ current (IK, IR) (IC₅₀ = 10 nM).

Quality Level

100

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, desiccated (hygroscopic)

color

white to off-white

solubility

DMSO: 50 mg/mL, water: 50 mg/mL

shipped in

ambient

storage temp.

−20°C

SMILES string

[S](=O)(=O)(Nc1ccc(cc1)C(=O)C2CCN(CC2)CCc3nc(ccc3)C)C

InChI

1S/C21H27N3O3S/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

InChI key

SRUISGSHWFJION-UHFFFAOYSA-N

Description

General description

A potent and selective inhibitor of the inactivating inward-rectifying potassium current (IK,IR) (IC₅₀ = 10 nM). In inside-out patches, E-4031 also blocks ATP sensitive K⁺ channel (EC₅₀ = 31 µM). A specific blocker of cardiac HERG channels (IC₅₀ = 7.7 nM). A class III anti-arrhythmic agent with differential atrial versus ventricular activity.

A potent and selective inhibitor of the rapid type of inactivating inward-rectifying K⁺ current (IK, IR) (IC₅₀ = 10 nM). A class III anti-arrhythmic agent with differential atrial versus ventricular activity. A specific blocker of HERG channels (IC₅₀ = 7.7 nM).

Biochem/physiol Actions

Cell permeable: no

Primary Target
Inhibitor of the rapid type of inactivating inward-rectifying K+ current

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 10 nM inhibiting the rapid type of inactivating inward-rectifying K+ current

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Ficker, E., et al. 2000. Am. J. Physiol.279, H1748.
Ono, K., et al. 2000. J. Physiol. (London)524 (Pt. 1), 51.
Xie, J.T., et al. 2000. Methods Find. Exp. Clin. Pharmacol.22, 67.
Bauer, C.K., et al. 1999. Mol. Cell Endocrinol. 148, 37.
Baskin, E.P., and Lynch, J.J. 1998. J. Pharmacol. Exp. Ther. 285, 135.
Weinsberg, F., et al. 1997. Pflugers Arch. 434, 1.
West, P.D., et al. 1997. J. Cardiovasc. Pharmacol. Ther.2, 205.
West, P.D., et al. 1996. Pharmacol. Toxicol.78, 89.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c