324470

E-4031

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

• Synonim(y): E-4031, 4ʹ-[[1-[2-(6-Methyl-2-pyridinyl)ethyl-4-piperidinyl]carbonyl]methanesulfonanilide, 2HCl
• Wzór empiryczny (zapis Hilla): C₂₁H₂₇N₃O₃S · 2HCl · 2H₂O
• Numer CAS: 113558-89-7
• Masa cząsteczkowa: 510.47
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• product name: E-4031, A potent and selective inhibitor of the rapid type of inactivating inward-rectifying K⁺ current (IK, IR) (IC₅₀ = 10 nM).
• Poziom jakości: 100
• Próba: ≥98% (HPLC)
• Postać: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; desiccated (hygroscopic)
• kolor: white to off-white
• rozpuszczalność: DMSO: 50 mg/mL; water: 50 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: −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
• Klucz InChI: SRUISGSHWFJION-UHFFFAOYSA-N

Opis

Opis ogólny

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).

Działania biochem./fizjol.

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

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

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

Inne uwagi

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.

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 1
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable