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Pterinotoxin-1

β-Theraphotoxin-Pm1a, β-TRTX-Pm1a, Peptide A

A Novel Blocker of NaV1.3, NaV1.7, and NaV1.8 Voltage-Gated Na+ Channels

Cat #: STT-100
Alternative Name β-Theraphotoxin-Pm1a, β-TRTX-Pm1a, Peptide A
Lyophilized Powder yes
  • Bioassay Tested
    • Origin Synthetic peptide
    MW: 3970 Da
    Purity: >98% (HPLC)
    Effective concentration 2-5 µM.
    Sequence DDCLGMFSSCDPDNDKCCEGRKCNRKDKWCKYVL.
    Modifications Disulfide bonds between Cys3-Cys18, Cys10-Cys23, Cys17-Cys30. Leu34 – C-terminal amidation.
    Structure
    • This product is sold under license from Alomone Preclinical Ltd.
    Activity Pterinotoxin-1 inhibits rat voltage-gated Na+ channels NaV1.3, NaV1.7 and NaV1.8.
    Accession number B3EWN0.
    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 20 mM ammonium acetate, pH =6. 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 Pterinotoxin-1 inhibits rat NaV1.3 and NaV1.8 channels heterologously expressed in HEK and ND7-23 cells, respectively.
      Alomone Labs Pterinotoxin-1 inhibits rat NaV1.3 and NaV1.8 channels heterologously expressed in HEK and ND7-23 cells, respectively.
      A. Dose response of NaV channels inhibition by Pterinotoxin-1 (#STT-100). The inhibition was measured in 3-5 cells for each dose in rat NaV1.3 channels expressed in HEK cells and 3-5 cells for rat NaV1.8 expressed in ND7-23 cells (in the presence of 600 nM Tetrodotoxin citrate (#T-550)). B. Example of superimposed current traces of rat NaV1.3 channel activity before and during application of 2 µM of Pterinotoxin-1. 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. C. Example of superimposed current traces of rat NaV1.8 channel activity before and during application of 2 µM of Pterinotoxin-1 (both in the presence of 600 nM Tetrodotoxin (with citrate)). The same voltage protocol was used as in graph B.
    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. Sheets, P.L. et al. (2008) J. Pharmacol. Exp. Ther. 326, 89.
    3. Zimmermann, K. et al. (2007) Nature 447, 855.
    4. Amir, E. et al. (2006) J. Pain 7, S1.
    Scientific background

    Pterinotoxin-1 is isolated from the Pterinochilus murinus (Usambara) spider venom and is a synthetic version of the peptide1.

    Pterinotoxin-1 inhibits voltage-gated rat NaV1.3, NaV1.7 and NaV1.8 Na+ channels.

    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 therapeutics2-3.

    The expression and functional properties of NaV channels in peripheral sensory neurons can be dynamically regulated following axonal injury or peripheral inflammation4.

    Pterinotoxin-1 shows high homology to Phrixotoxin-3 (#STP-720) (58%), Huwentoxin-IV (#STH-100) (50%) and Ceratotoxin-2 (#STC-100) (66%).

    Target NaV channels
    Peptide Content: 100%
    Lyophilized Powder
    Last update: 06/11/2022

    Pterinotoxin-1 (#STT-100) is a highly pure, synthetic, and biologically active peptide toxin.

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    For research purposes only, not for human use
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