GpTx-1

A Blocker of NaV1.7, NaV1.5 and NaV1.4 Na+ Channels
    Cat #: STG-400
  • Lyophilized Powder
  • Bioassay Tested
  • Origin Synthetic peptide
    MW: 4073.9 Da.
    Purity: >98% (HPLC)
    Effective concentration 10-200 nM.
    Sequence DCLGFMRKCIPDNDKCCRPNLVCSRTHKWCKYVF.
    Modifications Disulfide bonds between Cys2-Cys17, Cys9-Cys23, and Cys16-Cys30.  Phe34 – C-terminal amidation.
    Structure
    • GpTx-1
    Molecular formula C176H271N53O45S7.
    Activity GpTx-1 is a NaV1.7, NaV1.5 and NaV1.4 Na+ channel blocker1,2.
    References-Activity
    1. Murray, J.K. et al. (2015) J. Med. Chem. 58, 2299.
    2. Murray, J.K. et al. (2015) Bioorg. Med. Chem. Lett. 25, 4866.
    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 other aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to two weeks at 4°C or three months at -20°C.
    Our bioassay
    • GpTx-1
      Alomone Labs GpTx-1 inhibits NaV1.7 channels expressed in Xenopus oocytes.
      A. Time course of GpTx-1 (#STG-400) inhibition of NaV1.7 channels current. Membrane potential was held at -100 mV, current was elicited by a 100 ms voltage step to 0 mV every 10 sec, and inhibited by 200 nM GpTx-1 (bar), applied for 10 min. B. Superimposed traces of NaV1.7 channel currents upon application of control and of 200 nM GpTx-1 (as indicated), taken from the recording shown in A.
    References - Scientific background
    1. Murray, J.K. et al. (2015) J. Med. Chem. 58, 2299.
    2. Murray, J.K. et al. (2015) Bioorg. Med. Chem. Lett. 25, 4866.
    3. Chow, C.Y. et al. (2015) Toxins 7, 2494.
    4. Klint J.K. et al. (2015) Br. J. Pharmacol. 172, 2445.
    Scientific background

    GpTx-1 is a 34-residue peptide with inhibitory cystine knot motif and contains 3 important residues near the C-terminus that are critical for potently blocking NaV1.7 channel, with IC50 value of 10 nM. The peptide toxin was originally isolated from the Grammostola porteri spider venom1,2. In addition, GpTx-1 demonstrates selectivity against other NaV subtypes including NaV1.4 and NaV1.5 channels.

    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 are considered to be important therapeutic targets for a wide variety of pathophysiological conditions such as cardiac arrhythmia, and epilepsy. NaV1.7 channel plays an important role in human pain signalling pathway and it is an important therapeutic target for treatment of chronic pain3,4.

    Target NaV1.7, NaV1.5, NaV1.4 channels
    Net Peptide Content: 100%
    Last update: 24/01/2020

    GpTx-1 (#STG-400) is a highly pure, synthetic, and biologically active peptide toxin.

    For research purposes only, not for human use
    Shipping and Ordering information