324470

E-4031

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

• Sinônimo(s): E-4031, 4ʹ-[[1-[2-(6-Methyl-2-pyridinyl)ethyl-4-piperidinyl]carbonyl]methanesulfonanilide, 2HCl
• Fórmula empírica (Notação de Hill): C₂₁H₂₇N₃O₃S · 2HCl · 2H₂O
• Número CAS: 113558-89-7
• Peso molecular: 510.47
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• product name: E-4031, A potent and selective inhibitor of the rapid type of inactivating inward-rectifying K⁺ current (IK, IR) (IC₅₀ = 10 nM).
• Nível de qualidade: 100
• Ensaio: ≥98% (HPLC)
• forma: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; desiccated (hygroscopic)
• cor: white to off-white
• solubilidade: DMSO: 50 mg/mL; water: 50 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: −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
• chave InChI: SRUISGSHWFJION-UHFFFAOYSA-N

Descrição

Descrição geral

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).

Ações bioquímicas/fisiológicas

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

Advertência

Toxicity: Standard Handling (A)

Reconstituição

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

Outras notas

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.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 1
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable