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m3-Huwentoxin IV

Mutated Huwentoxin-IV, Triple-mutated Huwentoxin-IV, m3-HwTx-IV, m3-Huwentoxin-IV

A Potent and Selective NaV1.7 Channel Blocker

Cat #: STH-102
Alternative Name Mutated Huwentoxin-IV, Triple-mutated Huwentoxin-IV, m3-HwTx-IV, m3-Huwentoxin-IV
Lyophilized Powder yes
  • Bioassay Tested
    • Origin Synthetic peptide
    MW: 3988 Da
    Purity: >98% (HPLC)
    Form Lyophilized powder.
    Effective concentration 3-100 nM.
    Sequence GCLGIFKACNPSNDQCCKSSKLVCSRKTRWCKWQI.
    Modifications Disulfide bonds between Cys2-Cys17, Cys9-Cys24, and Cys16-Cys31. Ile35 - C-terminal amidation.
    Structure
    Molecular formula C170H271N53O46S6.
    Activity m3-Huwentoxin IV is a mutated form of the Huwentoxin IV with significant increased potency towards NaV1.7, displaying an IC50 value of 0.4 nM1.
    References-Activity
    1. Rahnama, S. et al. (2017) PLoS One 12, e0173551.
    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 for 5 min).
    Storage of solutions Up to two weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs m3-Huwentoxin IV blocks NaV1.7 channels expressed in Xenopus oocytes.
      Alomone Labs m3-Huwentoxin IV blocks NaV1.7 channels expressed in Xenopus oocytes.
      A. Representative time course of m3-Huwentoxin IV (#STH-102) inhibition of NaV1.7 current. Membrane potential was held at -100 mV, current was elicited by a 100 ms voltage step to -10 mV every 10 sec, and gradually and irreversibly inhibited by 50 nM m3-Huwentoxin IV (green). B. Superimposed traces of NaV1.7 current after application of control (black) and of 50 nM m3-Huwentoxin IV (green). Taken from the recording in A.
    References - Scientific background
    1. Rahnama, S. et al. (2017) PLoS One 12, e0173551.
    2. Chow, C.Y. et al. Toxins (2015) 7, 2494.
    3. Klint J.K. et al. (2015) Br. J. Pharmacol. 172, 2445.
    Scientific background

    Huwentoxin IV is a peptide toxin originally isolated from the venom of the Chinese bird-eating spider Haplopelma schmitdi that acts as a potent and selective NaV1.7 channel blocker displaying an IC50 value of 26 nM1. m3-Huwentoxin IV is a mutated form of the toxin with significant increased potency towards NaV1.7, displaying an IC50 value of 0.4 nM1.

    There are nine mammalian subtypes of voltage-gated sodium (NaV) channels: NaV1.1–NaV1.9. These channels responsible for propagating action potentials in excitable cells and considered to be important therapeutic targets for a wide variety of pathophysiological conditions such as cardiac arrhythmia, and epilepsy2,3.

    NaV1.7 channel plays an important role in the human pain signaling pathway and it is an important therapeutic target for the treatment of chronic pain2,3.

    Target NaV1.7 channel
    Peptide Content: 100%
    Lyophilized Powder
    Last update: 08/06/2021

    m3-Huwentoxin IV (#STH-102) is a highly pure, synthetic, and biologically active peptide toxin. It is a mutated variant of Huwentoxin IV, a peptide toxin originally isolated from the Chinese bird-eating spider Haplopelma schmitdi venom. m3-Huwentoxin IV is a significantly more potent NaV1.7 channel bocker, displaying an IC50 value of 0.4 nM.

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    For research purposes only, not for human use
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