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3R12Rα-Pompilidotoxin

3R12Rα-PMTX

An Activator of NaV Channels

Cat #: P-176
Alternative Name 3R12Rα-PMTX
Lyophilized Powder yes
  • Bioassay Tested
  • Origin Synthetic peptide
    MW: 1586 Da.
    Purity: >98% (HPLC)
    Effective concentration 100-200 µM.
    Sequence RIRIGLFDQLSRL.
    Modifications Leu13 – C-terminal amidation.
    Structure
    Molecular formula C71H124N24O17.
    Activity 3R12Rα-PMTX slows NaV channel inactivation without changing the peak current-voltage relationship or the activation time course of the TTX-sensitive Na+ currents in the neuromuscular synapse1-3.
    References-Activity
    1. Schiavon, E. et al. (2010) FEBS J. 277, 918.
    2. Sahara, Y. et al. (2000) Eur. J. Neurosci. 12, 1961.
    3. Konno, K. et al. (2000) Neurosci. Lett. 285, 29.
    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
    • Alomone Labs 3R12Rα-PMTX enhances native NaV currents in ND7-23 cells.
      Alomone Labs 3R12Rα-PMTX enhances native NaV currents in ND7-23 cells.
      Native TTX-sensitive NaV currents in ND7-23 cells were elicited by a 50 ms voltage ramp from the holding potential of -100 mV to +60 mV, applied every 10 sec using whole-cell voltage clamp. A. Time course, showing the effect of 100 µM 3R12Rα-Pompilidotoxin (#P-176) application (horizontal bar) on current area, indicative of a toxin-dependent decrease in NaV currents inactivation. B. Superimposed traces of NaV currents in ND7-23 cells under control conditions and after 2 min perfusion with 100 µM 3R12Rα-Pompilidotoxin.
    References - Scientific background
    1. Schiavon, E. et al. (2010) FEBS J. 277, 918.
    2. Sahara, Y. et al. (2000) Eur. J. Neurosci. 12, 1961.
    3. Konno, K. et al. (2000) Neurosci. Lett. 285, 29.
    4. Konno, K. et al. (1998) Biochem Biophys. Res. Commun. 250, 612.
    5. Harsch, A. et al. (1998) Neurosci. Lett. 252, 49.
    Scientific background

    Pompilidotoxins (PMTX, α and β) are small peptides consisting of 13 amino acids.

    α-PMTX (#P-170) induces a unique pattern of repetitive action potentials previous seen with other neurotoxins and thus facilitate both excitatory and inhibitory synaptic transmission.

    Recently it was found that this toxin slows the Na+-channel inactivation, without changing the peak current-voltage relationship or the activation time course of the TTX-sensitive Na+ currents in the neuromuscular synapse of the lobster walking leg and in the rat trigeminal ganglion neurons2-4. Effective at concentrations of 10 nM in cultured rat cortical neurons5.

    3R12Rα-Pompilidotoxin (3R12Rα-PMTX) is a mutated form of the α-PMTX, originally isolated from the solitary wasp (Anoplius samariensis) venom1 and is a synthetic version of the peptide.

    3R12RKα-PMTX is mutated at position 3 as well as 12 with Lysine to Arginine transition, which enhanced its activity on voltage-gated Na+ channels 5-fold relative to α-PMTX1,3.

    Target NaV Na+ channels
    Net Peptide Content: 100%
    Last update: 02/03/2021

    3R12Rα-Pompilidotoxin (#P-176) is a highly pure, synthetic, and biologically active peptide toxin.

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