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Sigma-Aldrich

E-4031

≥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
UNSPSC Code:
12352200
NACRES:
NA.77

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

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

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

WGK

WGK 1

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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