Hainantoxin-III, Selective blocker of TTX-S VGSC Hainantoxin-III (HNTX-III) is a peptide that has been isolated from the venom of the Chinese bird spider Seleconosmia hainana. Hainantoxin-III specifically blocks mammalian neuronal tetrodotoxin-sensitive voltage-gated sodium channels (VGSCs). Hainantoxin III was found inactive on tetrodotoxin-resistant VGSCs and voltage-gated Ca2+ channels (both high and low voltage-activated). Hainantoxin-III strongly depressed the amplitude of rat DRG tetrodotoxin-sensitive Na+ currents with an IC50 value of 1.1 nM. Like Hainantoxin-IV, Hainantoxin-III causes a hyperpolarizing shift of about 10 mV in the voltage midpoint of steady-state Na+ channel inactivation. Similar to Huwentoxin-IV, Hainantoxin-III and Hainantoxin-IV do not affect the activation and inactivation kinetics of Na+ currents. Hainantoxin-III inhibits Nav1.7 current amplitude without significantly altering the activation and inactivation kinetics. Hainantoxin-III increases the deactivation of the Nav1.7 current after extreme depolarizations. Hainantoxin-III seems to interact with site 4 and to trap the domain II voltage sensor in the closed state. The inhibition of Nav1.7 by hainantoxin-III is reversible upon washing, but no reversibility was observed for Hainantoxin-IV and Huwentoxin-IV. Hainantoxin-III was shown to block Nav1.1, Nav1.2, Nav1.3 and Nav1.7 expressed in HEK293 cells with IC50 values of 1.27 µM, 275 nM, 491 nM and 232 nM, respectively. Hainantoxin-III technical information AA sequence: Gly-Cys2-Lys-Gly-Phe-Gly-Asp-Ser-Cys9-Thr-Pro-Gly-Lys-Asn-Glu-Cys16-Cys17-Pro-Asn-Tyr-Ala-Cys22-Ser-Ser-Lys-His-Lys-Trp-Cys29-Lys-Val-Tyr-Leu-NH2 Disulfide bonds: Cys2-Cys17, Cys9-Cys22, and Cys16-Cys29 Length (aa): 33 Formula: C154H228N44O45S6 Molecular Weight: 3608.20 Da Appearance: White lyophilized solid Solubility: water and saline buffer CAS number: Not available Source: Synthetic Purity rate: > 97% http://www.smartox-biotech.com/en/sodium-channel/283-hainantoxin-iii-sodium-channel-blocker

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