Huwentoxin-IV is a 35 amino acid peptidyl toxin isolated from the tarantula Haplopelma schmidti venom and its structure represents a typical cystine knot motif. Huwentoxin-IV acts selectively on tetrodotoxin-sensitive (TTX-S) voltage-gated Na+ channels, with an IC50 of 30 nM in rat DRG neurons. It preferentially inhibits central neuronal voltage-gated Na+ channel subtypes: hNav1.7 (IC50 of 26 nM), rNav1.2 (IC50 of 150 nM), and rNav1.3 (IC50 of 338 nM), compared with muscle subtypes rNav1.4 and hNav1.5 (IC50 is > 10 µM). Huwentoxin-IV inhibits Na+ channels by trapping the voltage sensor of domain II of the site 4 in the inward, closed configuration.
产品描述
A Potent Blocker of Neuronal TTX-Sensitive Voltage-Gated Na+ Channel
产品形式
Huwentoxin-IV is a 35 amino acid peptidyl toxin isolated from the tarantula Haplopelma schmidti venom and its structure represents a typical cystine knot motif. Huwentoxin-IV acts selectively on tetrodotoxin-sensitive (TTX-S) voltage-gated Na+ channels, with an IC50 of 30 nM in rat DRG neurons. It preferentially inhibits central neuronal voltage-gated Na+ channel subtypes: hNav1.7 (IC50 of 26 nM), rNav1.2 (IC50 of 150 nM), and rNav1.3 (IC50 of 338 nM), compared with muscle subtypes rNav1.4 and hNav1.5 (IC50 is > 10 µM). Huwentoxin-IV inhibits Na+ channels by trapping the voltage sensor of domain II of the site 4 in the inward, closed configuration.