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
• MDL number: MFCD07363980
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: solid
• Storage condition: OK to freeze, desiccated (hygroscopic)

Właściwości

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

Opis

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)

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Informacja o środkach bezpieczeństwa

• Klasa składowania: 11 - Combustible Solids
• wgk: WGK 1
• flash_point_f: Not applicable
• flash_point_c: Not applicable