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Alpha-conotoxin GeXIVA

αO-Conotoxin GeXIVA, Alpha-O-conotoxin GeXIVA, Conotoxin Ge14.1, Conotoxin GeXIVAWT

A Potent Antagonist of α9α10 nAChR, a Weak Antagonist of other nAChRs.

Cat #: STC-220
Alternative Name αO-Conotoxin GeXIVA, Alpha-O-conotoxin GeXIVA, Conotoxin Ge14.1, Conotoxin GeXIVAWT
Lyophilized Powder yes
  • Bioassay Tested
  • Origin Conus generalis (General cone)
    Source Synthetic Peptide
    MW: 3453 Da
    Purity: >98%
    Form Lyophilized Powder
    Effective concentration 5-20 nM
    Sequence TCRSSGRYCRSPYDRRRRYCRRITDACV-OH
    Modifications The native disulfide bond pairing has not been studied.
    Structure
    Molecular formula C139H227N55O41S4
    Activity A potent and selective antagonist of the α9α10 nAChR. GeXIVA exhibits analgesic activity in animal models of pain without the development of tolerance1-4.
    References-Activity
    1. Luo, S. et al. (2015) PNAS, 112, E4026.
    2. Li, X. et al. (2016) Prog. Neuro-Psychopharmacol. Biol. Psych., 66, 112.
    3. Zhangsun, D. et al. (2017) Neuropharmacol., 127, 243.
    4. Wang, H. et al. (2019), Mar. Drugs, 17, 265.
    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. Protect from light and moisture.
    Solubility Soluble in water.
    It is recommended to prepare fresh solutions in working buffers before use, or aliquot stock solutions reconstituted in distilled water and keep at -20°C. Upon use, dilute the stock solution in the desired working buffer. Prevent repeated thawing and freezing cycles. Centrifuge all product preparations before use (10,000 g for 5 min).
    Storage of solutions Store up to one week at 4°C or up to 6 months at -20°C.
    Our bioassay
    • Alomone Labs α-Conotoxin GeXIVA inhibits α7 nAChR heterologously expressed in Xenopus oocytes.
      Alomone Labs α-Conotoxin GeXIVA inhibits α7 nAChR heterologously expressed in Xenopus oocytes.
      A. Time course of α-Conotoxin GeXIVA (#STC-220) action on α7 nAChR currents, elicited every 50 sec by a transient application of 100 µM ACh + 0.3 µM PNU-120596, while membrane potential was held at -80 mV. Application of 100 nM (green) and 500 nM (magenta) α-Conotoxin GeXIVA significantly inhibits the currents.
      B. Superimposed traces of α7 nAChR currents upon application of control, 100nM (green) and 500 nM (magenta) α-Conotoxin GeXIVA (taken from the recording in A).
    References - Scientific background
    1. Luo, S. et al. (2015) PNAS, 112, E4026.
    2. Zhangsun, D. et al. (2017) Neuropharmacol., 127, 243.
    3. Wang, H. et al. (2019), Mar. Drugs, 17, 265.
    4. Li, X. et al. (2016) Prog. Neuro-Psychopharmacol. Biol. Psych., 66, 112.
    5. Sun, Z. et al. (2020) Mar. Drugs, 18, 195.
    6. Gotti, C. et al. (2009) Biochem. Pharmacol., 78, 703.
    7. Vincler, M. et al. (2006) PNAS, 103, 17880.
    8. Liu, Y. et al. (2019) Mar. Drugs, 17, 256.
    Scientific background

    α-conotoxin GeXIVA (αO-conotoxin GeXIVA or GeXIVA) is a 28 amino acid peptidyl toxin, which was discovered from a transcriptome analysis of the South China Sea mollusk, Conus generalis1. GeXIVA belongs to the O1-gene superfamily and is a potent and selective antagonist of the α9α10 nicotinic acetylcholine receptor (nAChR) subtype1. The toxin-mediated blockade of α9α10 nAChRs is voltage-dependent, suggesting that the toxin binding site might be allosterically coupled to a voltage-sensitive domain of the nAChR1,2. GeXIVA exhibits analgesic activity in animal models of pain without the development of tolerance1-4.

    nAChRs are involved in a wide range of physiological functions in the central and peripheral nervous systems.  Alterations in nAChR expression and/or function are associated with a number of pathophysiological conditions including pain, addiction, epilepsy, autism, schizophrenia, Alzheimer's and Parkinson's diseases, as well as many types of cancers2,6. The nAChRs are formed from the assembly of five homologous subunits and neuronal nAChRs are assembled from a combination of α- and β-subunits. They share a common basic structure, but their pharmacological and functional properties arise from the wide range of different subunit combinations which generate distinctive subtypes6. The α9α10 nAChR subtype is a potential target for treating chronic pain, wound healing, the pathophysiology of the auditory system, and various cancers4-7. GeXIVA potently alleviated neuropathic pain in several rat models1-4 and also exhibited an antitumor effect5,8.

    Target α9α10 nAChRs
    Peptide Content: 100%
    Last update: 13/06/2021

    αO-Conotoxin GeXIVA (#STC-220) is a highly pure, synthetic, and biologically active peptide toxin.

    For research purposes only, not for human use
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