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

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Acid-Sensing Ion Channel 3 Blocker, ASIC3 Channel Blocker

Primary Target: ASIC3
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₉₆H₂₈₀N₅₄O₆₁S₆

Products

Catalog NumberPackaging Qty/Pack
5.00527.0001 Glass bottle 100 μg
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 Protect from light
-20°C
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.