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

500527
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₉₆H₂₈₀N₅₄O₆₁S₆

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.00527.0001
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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
          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

          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.