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Huwentoxin-IV

Names

[ CAS No. ]:
526224-73-7

[ Name ]:
Huwentoxin-IV

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Sodium Channel
Research Areas >> Neurological Disease

[Target]

IC50: 26 nM (Nav1.7), 150 nM (Nav1.2), 338 nM (Nav1.3), 400 nM (Nav1.4)[1]


[References]

[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.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C174H278N52O51S6

[ Molecular Weight ]:
4106.78

Related Compounds