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324470 E-4031 - CAS 113558-89-7 - Calbiochem

324470
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Key Spec Table

Empirical FormulaCAS #
C₂₁H₂₇N₃O₃S · 2HCl · 2H₂O113558-89-7

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324470-5MGCN
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      Description
      OverviewA 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).
      Catalogue Number324470
      Brand Family Calbiochem®
      Synonyms4ʹ-[[1-[2-(6-Methyl-2-pyridinyl)ethyl-4-piperidinyl]carbonyl]methanesulfonanilide, 2HCl
      References
      ReferencesFicker, 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.
      Product Information
      CAS number113558-89-7
      ATP CompetitiveN
      FormWhite to off-white solid
      Hill FormulaC₂₁H₂₇N₃O₃S · 2HCl · 2H₂O
      Chemical formulaC₂₁H₂₇N₃O₃S · 2HCl · 2H₂O
      Hygroscopic Hygroscopic
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetInhibitor of the rapid type of inactivating inward-rectifying K+ current
      Primary Target IC<sub>50</sub>10 nM inhibiting the rapid type of inactivating inward-rectifying K+ current
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableN
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage -20°C
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      E-4031 - CAS 113558-89-7 - Calbiochem Certificates of Analysis

      TitleLot Number
      324470

      References

      Reference overview
      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.

      Citations

      Title
    • Jun Guo, Hongying Gang and Shetuan Zhang. (2006) Molecular Determinants of Cocaine Block of Human Ether-a-go-go-Related Gene Potassium Channels. Journal of Pharmacology and Experimental Therapeutics 317, 865-874.
    • Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision10-December-2016 JSW
      Synonyms4ʹ-[[1-[2-(6-Methyl-2-pyridinyl)ethyl-4-piperidinyl]carbonyl]methanesulfonanilide, 2HCl
      DescriptionA 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.
      FormWhite to off-white solid
      CAS number113558-89-7
      Chemical formulaC₂₁H₂₇N₃O₃S · 2HCl · 2H₂O
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml) or H₂O (50 mg/ml)
      Storage -20°C
      Hygroscopic
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesFicker, 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.
      Citation
    • Jun Guo, Hongying Gang and Shetuan Zhang. (2006) Molecular Determinants of Cocaine Block of Human Ether-a-go-go-Related Gene Potassium Channels. Journal of Pharmacology and Experimental Therapeutics 317, 865-874.