Huwentoxin-IV is a potent and selective sodium channel blocker that inhibits neuronal Nav1.7, Nav1.2, Nav1.3, and Nav1.4. It preferentially blocks the peripheral nerve subtype Nav1.7 by binding to neurotoxin receptor site 4. This compound has demonstrated analgesic effects in animal models of inflammatory and neuropathic pain. Its molecular weight is 4106.78, with a chemical formula of C174H278N52O51S6.
- Inhibits Nav1.7 with an IC50 of 26 nM
- Inhibits Nav1.2 with an IC50 of 150 nM
- Inhibits Nav1.3 with an IC50 of 338 nM
- Inhibits Nav1.4 with an IC50 of 400 nM
- Features sequence: Glu-Cys-Leu-Glu-Ile-Phe-Lys-Ala-Cys-Asn-Pro-Ser-Asn-Asp-Gln-Cys-Cys-Lys-Ss-Lys-Leu-Val-Cys-Ser-Arg-Lys-Thr-Trp-Cys-Lys-Tyr-Gln-Ile-NH2
- Includes disulfide bridges: Cys2-Cys17; Cys9-Cys24; Cys16-Cys31