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 |
Preparing Stock Solutions
The following data is based on the product molecular weight 4106.79. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 0.24 mL | 1.22 mL | 2.43 mL |
| 5 mM | 0.05 mL | 0.24 mL | 0.49 mL |
| 10 mM | 0.02 mL | 0.12 mL | 0.24 mL |
| 50 mM | 0 mL | 0.02 mL | 0.05 mL |
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References
References are publications that support the products' biological activity.
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
Keywords: Huwentoxin IV, supplier, Huwentoxin, 4, sodium, channels, NaV1.7, blockers, antagonists, toxins, voltage, gated, Na+, channels, selective, venoms, Voltage-gated, Sodium, Channels, Voltage-gated, Sodium, Channels, Tocris Bioscience
