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GTx1-15

ω/β-Theraphotoxin-Ps2a, β-TRTX-Ps2a, Peptide E

 A Blocker of Voltage-Gated Na+ and T-Type Ca2+ Channels

Cat #: STT-300
Alternative Name ω/β-Theraphotoxin-Ps2a, β-TRTX-Ps2a, Peptide E
Lyophilized Powder yes
  • Bioassay Tested
  • Origin Synthetic peptide
    MW: 4075 Da
    Purity: >98% (HPLC)
    Effective concentration 200-500 nM.
    Sequence DCLGFMRKCIPDNDKCCRPNLVCSRTHKWCKYVF.
    Modifications Disulfide bonds between Cys2-Cys17, Cys9-Cys23, Cys16-Cys30, Phe34 - C-terminal amidation.
    Structure
    • This product is sold under license from Alomone Preclinical Ltd.
    Molecular formula C176H271N53O45S7.
    Activity GTx1-15 inhibits rat NaV1.3 and NaV1.7 voltage-gated Na+ channels as well as T-type Ca2+ channels.
    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, pH > 8. 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
    • Alomone Labs GTx1-15 inhibits rat NaV1.3 channels heterologously expressed in HEK-293 cells.
      Alomone Labs GTx1-15 inhibits rat NaV1.3 channels heterologously expressed in HEK-293 cells.
      A. Dose-response of NaV1.3 channel inhibition by GTx1-15 (#STT-300). The inhibition was measured in 3-5 cells for each dose. B. Example of superimposed current traces of rat NaV1.3 channel activity before and during application of 0.3 µM of GTx1-15. Holding potential was -100 mV and currents were stimulated every 10 seconds by a voltage ramp of 40 msec from holding potential to +60 mV.
    References - Scientific background
    1. Meir, A., Cherki, R.S., Kolb, E., Langut, Y., Bajayo, N., 2011. Novel peptides isolated from spider venom, and uses thereof. U.S. Patent Application Publication # US 2011/0065647 A1.
    2. Ono, S. et al. (2011) Toxicon. 58, 265.
    3. Sheets, P.L. et al. (2008) J. Pharmacol. Exp. Ther. 326, 89.
    4. Zimmermann, K. et al. (2007) Nature 447, 855.
    5. Amir, R. et al. (2006) J. Pain 7, S1.
    Scientific background

    GTx1-15 is isolated from the Grammostola rosea (Phrixotrichus auratus) spider venom and is a synthetic version of the peptide1,2.

    GTx1-15 inhibits voltage-gated rat NaV1.3 and NaV1.7 Na+ channels, as well as T-type Ca2+ channels1,2.

    Voltage-gated Na+ channels (VGSC, NaV) play a critical role in excitability of nociceptors (pain-sensing neurons).

    The peripheral-specific Na+ channels NaV1.7, NaV1.8 and NaV1.9 are particularly important in the pathophysiology of different pain syndromes and hence, thought to be potential targets for pain therapeutics3-4. The expression and functional properties of NaV channels in peripheral sensory neurons can be dynamically regulated following axonal injury or peripheral inflammation5.

    GTx1-15 shows high homology to Phrixotoxin-3 (#STP-720) (76%) and Ceratotoxin-2 (#STC-100) (57%).

    Target NaV Na+ Channels, T-type Ca2+ channels
    Peptide Content: 100%
    Last update: 29/08/2021

    GTx1-15 (#STT-300) is a highly pure, synthetic, and biologically active peptide toxin.

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