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Heteropodatoxin-1

Kappa-sparatoxin-Hv1a, Kappa-SPRTX-Hv1a, HpTX1, Toxin AU3/KJ5

An activator of Nav1.9 and an inhibitor of Kv4.2 and Nav1.7

Cat #: STH-320
Alternative Name Kappa-sparatoxin-Hv1a, Kappa-SPRTX-Hv1a, HpTX1, Toxin AU3/KJ5
Lyophilized Powder yes
  • Bioassay Tested
  • Origin Heteropoda venatoria (Brown huntsman spider)
    Source Synthetic
    MW: 3910.4 Da
    Purity: >98%
    Form Lyophilized powder
    Effective concentration 0.5-5 µM
    Sequence DCGTIWHYCGTDQSECCEGWKCSRQLCKYVIDW-NH2
    Modifications Disulfide bonds between: Cys2-Cys17, Cys9-Cys22, Cys16-Cys27
    Trp33 – amidation
    Structure
    Molecular formula C168H237N45O52S6
    Activity Heteropodatoxin-1, first identified as an inhibitor of Kv4.2 voltage gated potassium channel, also inhibits Nav1.7 and activates Nav1.9 channels, but does not affect Nav1.8 channels.
    References-Activity
    1. Sanguinetti, M.C. et al. (1997) Mol. Pharmacol. 51, 491.
    2. Zhou X. et al. (2020) Nature Comm. Vol. 11, 2293.
    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 Soluble in DDW. Centrifuge all products before use (10000 x g 5 min).
    Storage of solutions Store at 4°C for up to 1 week. For longer periods, small aliquots should be stored at -20°C. Avoid multiple freezing and thawing.
    Our bioassay
    • Alomone Labs Heteropodatoxin-1 inhibits NaV1.7 channel currents heterologously expressed in Xenopus oocytes.
      Alomone Labs Heteropodatoxin-1 inhibits NaV1.7 channel currents heterologously expressed in Xenopus oocytes.
      A. Representative time course of Heteropodatoxin-1 (#STH-320) inhibition of NaV1.7 channels current. Membrane potential was held at -100 mV, current was elicited by a 100 ms voltage step to -10 mV every 10 sec, and significantly inhibited by application of 4 µM
      Heteropodatoxin-1 (green).
      B. Superimposed traces of NaV1.7 channel current in the absence (control) and presence (green) of 4 µM Heteropodatoxin-1 (taken from the recording in A).
    References - Scientific background
    1. Sanguinetti, M.C. et al. (1997) Mol. Pharmacol. 51, 491.
    2. Zhou X. et al. (2020) Nature Comm. Vol. 11, 2293.
    3. Dib-Hajj. S.D. et al. (2010) Annu. Rev. Neurosci. 33, 325.
    Scientific background

    Heteropodatoxin-1 (HpTX1 or kappa-sparatoxin-Hv1a) is a peptide toxin originally isolated from Heteropoda venatoria, a spider species that is mostly present in tropical regions of the world. This toxin belongs to the Heteropoda toxins family that includes HpTX1, HpTX2 and HpTX3, all of which were shown to be Kv4.2 voltage gated potassium channel inhibitors1.

    Recently it has been found that HpTX1 is a Nav channel pharmacological tool as well. HpTX1 inhibits Nav1.7 and activates Nav1.9, but has no effect on Nav1.8 channel2.

    The voltage-gated sodium channels Nav1.7, Nav1.8 and Nav1.9, preferentially expressed in the peripheral terminals of sensory neurons and are critical for pain perception in peripheral nociceptors3. Loss of function of Nav1.7 leads to congenital insensitivity to pain in humans2. Genetic and functional studies have illustrated that mutations in Nav1.8 and Nav1.9 cause human pain disorders, providing direct clinical evidence linking these two channels to human pain. Considering that the three channels play distinct roles in the generation and propagation of action potentials, they might regulate pain signaling cooperatively. HpTx1-induced hypersensitivity is mediated by Nav1.9 activation and offers pharmacological insight into the relationship of the three Nav channels in pain signaling2.

    Target Nav1.9, Nav1.7 and Kv4.2
    Net Peptide Content: 100%

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    Last update: 26/01/2021

    Heteropodatoxin-1 (#STH-320) is a highly pure, synthetic and biologically active peptide toxin.

    For research purposes only, not for human use

    Applications

    Specifications

    Scientific Background

    Citations

    Citations
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