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APETx2

Toxin APETx2, Pi-AITX-Ael2b, Pi-actitoxin-Ael2b

A Blocker of ASIC3 Channel

Cat #: STA-160
Alternative Name Toxin APETx2, Pi-AITX-Ael2b, Pi-actitoxin-Ael2b
Lyophilized Powder yes
  • Bioassay Tested
    • Origin Synthetic peptide
    MW: 4561 Da
    Purity: >98% (HPLC)
    Effective concentration 10 nM - 3 µM.
    Sequence GTACSCGNSKGIYWFYRPSCPTDRGYTGSCRYFLGTCCTPAD.
    Modifications Disulfide bonds between Cys4-Cys37, Cys6-Cys30 and Cys20-Cys38.
    Structure
    Molecular formula C196H280N54O61S6.
    CAS No.: 713544-47-9
    Activity APETx2 inhibits ASIC3 channels1.
    References-Activity
    1. Chagot, B. et al. (2005) Protein Sci. 14, 2003.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Any aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to one week at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs APETx2 inhibits ASIC3 channels expressed in Xenopus oocytes.
      Alomone Labs APETx2 inhibits ASIC3 channels expressed in Xenopus oocytes.
      A.Time course of APETx2 (#STA-160) inhibition of ASIC3 channels current. Membrane potential was held at -60 mV, current was elicited every 50 sec by a transient applications of pH 5.5, and was inhibited significantly by 4 min applications of 0.5 µM and 1 µM APETx2, as indicated by horizontal bars. B.Superimposed traces of ASIC3 currents upon application of control, 0.5 µM and 1 µM APETx2 (taken from the experiment in A).
    References - Scientific background
    1. Diochot, S. et al. (2004) EMBO J. 23, 1516.
    2. Chagot, B. et al. (2005) Protein Sci. 14, 2003.
    3. Gao, M. et al. (2016) Eur. J. Ortho. 38, 577.
    4. Yan, J. et al. (2013) Headache 53, 1250.
    5. Izumi, M. et al. (2012) J. Biomed. Sci. 19, 77.
    Scientific background

    Natural APETx2 is a 42-amino-acid peptidyl toxin, originally isolated from the sea anemone Anthopleura elegantissima. APETx2 was shown to be a selective, potent and reversible blocker of the homodimer proton gated channel ASIC3. ASIC3 has been implicated in pain transduction associated with acidosis in inflamed or ischemic tissues. APETx2 directly inhibits the ASIC3 channel by acting at its external side of the channel in a pH dependent manner.

    APETx2 also inhibits the hetromer ASIC2b-ASIC3 channel but does not inhibit the activity of ASIC1 isoform1.

    Structurally APETx2 is related to APETx1 a toxin that targets HERG K+ channel1,2.

    Target ASIC3 channels
    Net Peptide Content: 100%
    Lyophilized Powder
    Last update: 08/06/2021

    APETx2 (#STA-160) is a highly pure, synthetic, and biologically active peptide toxin.

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    For research purposes only, not for human use

    Applications

    Specifications

    Scientific Background

    Citations

    Citations
    Product citations
    1. Su, Y.S. et al. (2018) Neuropharmacology 130, 92.
    2. Zhou, R.P. et al. (2018) Gene 642, 230.
    3. Burgos-Vega, C.C. et al. (2016) Pain 157, 2722.
    4. Cao, Q. et al. (2016) Mol. Neurobiol. 53, 485.
    5. Fu, H. et al. (2016) Clin. Exp. Pharmacol. Physiol. 43, 193.
    6. Gao, M. et al. (2016) Eur. J. Ortho. 38, 577.
    7. Xu, X.X. et al. (2016) Eur. J. Pain 20, 552.
    8. Yu, X.W. et al. (2015) Glia 63, 483.
    9. Chen, W.N. and Chen, C.C. (2014) Mol. Pain 10, 30.
    10. Martinez-Rojas, V.A. et al. (2014) Pharmacol. Rep. 66, 964.
    11. Radu, B.M. et al. (2014) Cell Biochem. Biophys. 68, 9.
    12. Yan, J. et al. (2013) Headache 53, 1250.
    13. Izumi, M. et al. (2012) J. Biomed. Sci. 19, 77.

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