526224-73-7
Chemical Structure
Huwentoxin-IV
- CAS No.: 526224-73-7
- Formula:C174H278N52O51S6
- Molecular Weight:4106.78
SMILES: O=C(N[C@@H](CSSC[C@@H](C(N[C@@H](CCCCN)C(N[C@@H](CO)C(N[C@@H](CO)C(N[C@@H](CCCCN)C(N[C@@H](CC(C)C)C(N[C@H]1C(C)C)=O)=O)=O)=O)=O)=O)NC2=O)C(N[C@@H](CC(C)C)C(N[C@@H](CCC(O)=O)C(N[C@@H]([C@@H](C)CC)C(N[C@@H](CC3=CC=CC=C3)C(N[C@@H](CCCCN)C(N[C@@H](C)C(N[C@@H](CSSC[C@@H](C(N[C@@H](CO)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCCN)C(N[C@@H]([C@H](O)C)C(N[C@@H](CCCNC(N)=N)C(N[C@H]4CC5=CNC6=CC=CC=C56)=O)=O)=O)=O)=O)=O)NC1=O)C(N[C@@H](CC(N)=O)C(N7[C@@H](CCC7)C(N[C@@H](CO)C(N[C@@H](CC(N)=O)C(N[C@@H](CC(O)=O)C(N[C@@H](CCC(N)=O)C(N[C@H]2CSSC[C@@H](C(N[C@@H](CCCCN)C(N[C@@H](CC8=CC=C(C=C8)O)C(N[C@@H](CCC(N)=O)C(N[C@@H]([C@@H](C)CC)C(N)=O)=O)=O)=O)=O)NC4=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@H](CCC(O)=O)N
Biological Activity: Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain[1][2].
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Huwentoxin-IV | Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain. | |||||||||||||||||||||
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References
- [1]. Xiao Y, et, al. 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. 2008 Oct 3;283(40):27300-13. [Content Brief]
- [2]. Liu Y, et, al. Analgesic effects of Huwentoxin-IV on animal models of inflammatory and neuropathic pain. Protein Pept Lett. 2014; 21(2): 153-8. [Content Brief]
