324470
E-4031
≥98% (HPLC), solid, K⁺ current inhibitor, Calbiochem®
别名:
E-4031, 4ʹ-[[1-[2-(6-Methyl-2-pyridinyl)ethyl-4-piperidinyl]carbonyl]methanesulfonanilide, 2HCl
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关于此项目
经验公式（希尔记法）:
C21H27N3O3S · 2HCl · 2H2O
化学文摘社编号:
分子量:
510.47
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
产品名称
E-4031, A potent and selective inhibitor of the rapid type of inactivating inward-rectifying K+ current (IK, IR) (IC50 = 10 nM).
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
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
Quality Level
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
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.
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)
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
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