HUWENTOXIN IV

Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain[1][2].

Nav1.7: 26 nM (IC₅₀); Nav1.3: 338 nM (IC₅₀); Nav1.4: 400 nM (IC₅₀); Nav1.2: 150 nM (IC₅₀)

[1] Xiao Y, et, al. Tarantula huwentoxin-IV inhibits neuronal sodium channels by binding to receptor site 4 and trapping the domain ii voltage sensor in the closed configuration. J Biol Chem. 2008 Oct 3;283(40):27300-13. DOI:10.1074/jbc.M708447200
[2] Liu Y, et, al. Analgesic effects of Huwentoxin-IV on animal models of inflammatory and neuropathic pain. Protein Pept Lett. 2014; 21(2): 153-8. DOI:10.2174/09298665113206660119