Huwentoxin IV

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Cat.No. 4718 - Huwentoxin IV | Glu-Cys-Leu-Glu-Ile-Phe-Lys-Ala-Cys-Asn-Pro-Ser-Asn-Asp-Gln-Cys-Cys-Lys-Ser-Ser-Lys-Leu-Val-Cys-Ser-Arg-Lys-Thr-Arg-Trp-Cys-Lys-Tyr-Gln-Ile-NH2 | CAS No. 526224-73-7
Description: Selective NaV1.7 channel blocker
Datasheet
Citations
Reviews
Literature

Biological Activity

Selective NaV1.7 channel blocker. Preferentially inhibits neuronal NaV1.7, 1.2 and 1.3 (IC50 values are 26, 150 and 338 nM respectively), compared to muscle subtypes NaV1.4 and 1.5 (IC50 = >10 μM). Inhibits the channel by binding at the neurotoxin receptor site 4 in the S3-S4 linker of domain II, trapping the voltage sensor in the inward, closed configuration.

Technical Data

M. Wt 4106.79
Formula C174H278N52O51S6
Sequence ECLEIFKACNPSNDQCCKSSKLVCSRKTRWCKYQI

(Modifications: Disulfide bridge: 2-17,9-24,16-31)

(Modifications: Ile-35 = C-terminal amide)

Storage Store at -20°C
CAS Number 526224-73-7
PubChem ID 90488968
InChI Key MJMLBAPXMAOKDU-UHFFFAOYSA-N
Smiles [H]N[C@@H](CCC(O)=O)C(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CC4=CNC5=C4C=CC=C5)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC4=CC=CC=C4)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC1=O)[C@@H](C)CC)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N3)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC2=O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)CC)C(N)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solubility Soluble to 1 mg/ml in water

References

References are publications that support the biological activity of the product.

Xiao et al (2008) 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. 283 27300 PMID: 18628201

Xiao et al (2011) Common molecular determinants of tarantula huwentoxin-IV inhibition of Na+ channel voltage sensors in domains II and IV. J.Biol.Chem. 286 27301 PMID: 21659528


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Keywords: Huwentoxin IV, Huwentoxin IV supplier, Huwentoxin, 4, sodium, channels, NaV1.7, blockers, antagonists, toxins, voltage, gated, Na+, selective, venoms, Voltage-gated, Sodium, Channels, 4718, Tocris Bioscience

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