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500527 APETx2, Anthopleura elegantissima, Recombinant, E. coli - Calbiochem

500527
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₉₆H₂₈₀N₅₄O₆₁S₆

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      Glass bottle 100 μg
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      Description
      OverviewOriginally isolated from sea anemone Anthopleura elegantissima, the 42 amino-acid toxin APETx2 is shown to block acidification-induced activation of homotrimeric acid-sensing ion channel composed of rat or human ASIC3, but not rat ASIC1a, ASIC1b, or ASIC2a, in a reversible manner. APETx2 is also shown to inhibit the Na+-dependent, alkalization-induced "nonconventional" channel activity seen in human, but not rat, ASIC3. APETx2 in vivo efficacy is demonstrated in various rat pain induction models (100 µL 2.2 µM APETx2 via i.m. injection). Reported to display much reduced potency against Kv3.4 and little or no effect toward hERG, Kv2.2, Kv3.1, Kv4.2, or Kv4.3 channel activity.
      Catalogue Number500527
      Brand Family Calbiochem®
      SynonymsAcid-Sensing Ion Channel 3 Blocker, ASIC3 Channel Blocker
      References
      ReferencesDelaunay, A., et al. 2012. Proc. Natl. Acad. Sci. 109, 13124.
      Sherwood, T.W., et al. 2012. Am. J. Physiol. Cell Physiol. 303, C699.
      Karczewski, J., et al. 2010. Br J Pharmacol. 161, 950.
      Chagot, B., et al. 2005. Protein Sci. 14, 2003.
      Diochot, S., et al. 2004. EMBO J. 23, 1516.
      Product Information
      FormLyophilized powder
      FormulationSupplied as a trifluoroacetate salt.
      Hill FormulaC₁₉₆H₂₈₀N₅₄O₆₁S₆
      Chemical formulaC₁₉₆H₂₈₀N₅₄O₆₁S₆
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetASIC3
      Primary Target IC<sub>50</sub>63 nM
      Purity≥95% by HPLC
      Physicochemical Information
      Peptide SequenceH-Gly-Thr-Ala-Cys⁴-Ser-Cys⁶-Gly-Asn-Ser-Lys-Gly-Ile-Tyr-Trp-Phe-Tyr-Arg-Pro-Ser-Cys²⁰-Pro-Thr-Asp-Arg-Gly-Tyr-Thr-Gly-Ser-Cys³⁰-Arg-Tyr-Phe-Leu-Gly-Thr-Cys³⁷-Cys³⁸-Thr-Pro-Ala-Asp-OH (disulfide bonds: 4 → 37, 6 → 30, 20 → 38)
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      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
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      APETx2, Anthopleura elegantissima, Recombinant, E. coli - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Delaunay, A., et al. 2012. Proc. Natl. Acad. Sci. 109, 13124.
      Sherwood, T.W., et al. 2012. Am. J. Physiol. Cell Physiol. 303, C699.
      Karczewski, J., et al. 2010. Br J Pharmacol. 161, 950.
      Chagot, B., et al. 2005. Protein Sci. 14, 2003.
      Diochot, S., et al. 2004. EMBO J. 23, 1516.
      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.

      Revision17-July-2013 JSW
      SynonymsAcid-Sensing Ion Channel 3 Blocker, ASIC3 Channel Blocker
      DescriptionOriginally isolated from sea anemone Anthopleura elegantissima, the 42 amino-acid toxin APETx2 is shown to block acidification-induced activation of homotrimeric acid-sensing ion channel composed of rat or human ASIC3 (IC50 against pH 7.4 to 6 ramping-induced transient current = 63 nM and 175 nM by whole-cell patch-clamp using COS cells expressing respective channel), but not rat ASIC1a, ASIC1b, or ASIC2a, in a reversible manner, presumably via its N-terminus interaction with type I β turn that connects β-strands I&II in the ASIC3 extracellular β-ball region. In addition to acidification-induced classical transient current, APETx2 is also shown to inhibit the Na+-dependent, alkalization-induced nonconventional channel activity seen in human, but not rat, ASIC3 (complete inhibition by 1 µM APETx3; pH 8.0). APETx2 in vivo efficacy is demonstrated in various rat pain induction models, including acid- (via calf i.m. injection of 100 µL pH 4.0 saline on day 1&5) induced mechanical hypersensitivity (pain withdrawal threshold = 76% and 24% of control rats with or without 100 µL 2.2 µM APETx2 i.m. injection prior to the second pH 4.0 saline injection). Although structurally related to known K+ channel modulators APETx1 and BDS-1/II, APETx2 is reported to display much reduced potency against Kv3.4 (38% inhibition by 3 µM APETx2) and little or no effect toward hERG, Kv2.2, Kv3.1, Kv4.2, or Kv4.3 channel activity.
      FormLyophilized powder
      FormulationSupplied as a trifluoroacetate salt.
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₉₆H₂₈₀N₅₄O₆₁S₆
      Peptide SequenceH-Gly-Thr-Ala-Cys⁴-Ser-Cys⁶-Gly-Asn-Ser-Lys-Gly-Ile-Tyr-Trp-Phe-Tyr-Arg-Pro-Ser-Cys²⁰-Pro-Thr-Asp-Arg-Gly-Tyr-Thr-Gly-Ser-Cys³⁰-Arg-Tyr-Phe-Leu-Gly-Thr-Cys³⁷-Cys³⁸-Thr-Pro-Ala-Asp-OH (disulfide bonds: 4 → 37, 6 → 30, 20 → 38)
      Purity≥95% by HPLC
      SolubilityAqueous buffer
      Storage -20°C
      Protect from light
      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
      ReferencesDelaunay, A., et al. 2012. Proc. Natl. Acad. Sci. 109, 13124.
      Sherwood, T.W., et al. 2012. Am. J. Physiol. Cell Physiol. 303, C699.
      Karczewski, J., et al. 2010. Br J Pharmacol. 161, 950.
      Chagot, B., et al. 2005. Protein Sci. 14, 2003.
      Diochot, S., et al. 2004. EMBO J. 23, 1516.