925463-91-8
Chemical Structure
Jingzhaotoxin-III
Synonym(s): β-TRTX-Cj1α
- CAS No.: 925463-91-8
- Formula:C174H241N47O46S6
- Molecular Weight:3919.45
SMILES: O=C(NCC(N[C@@H](CCC(O)=O)C(N[C@@H](CSSC[C@@H](C(N[C@@H](CCCCN)C(NCC(N[C@@H](CC1=CC=C(C=C1)O)C(N[C@H]2C)=O)=O)=O)=O)NC3=O)C(NCC(NCC(N[C@@H](CC4=CC=CC=C4)C(N[C@@H](CC5=CNC6=CC=CC=C56)C(N[C@@H](CC7=CNC8=CC=CC=C78)C(N[C@@H](CCCCN)C(N[C@@H](CSSC[C@@H](C(N[C@@H](CO)C(N[C@@H](CCCCN)C(N[C@@H]([C@H](O)C)C(N[C@@H](CC9=CNC%10=CC=CC=C9%10)C(NCC(N[C@H]%11CC%12=CNC%13=CC=CC=C%12%13)=O)=O)=O)=O)=O)=O)NC2=O)C(NCC(N[C@@H](CCCNC(N)=N)C(NCC(N[C@@H](CCCCN)C(N%14[C@@H](CCC%14)C(N%15[C@@H](CCC%15)C(N[C@H]3CSSC[C@@H](C(N[C@@H](C)C(N[C@@H](C(C)C)C(N[C@@H](CCC(O)=O)C(N[C@@H](C)C(N%16[C@@H](CCC%16)C(O)=O)=O)=O)=O)=O)=O)NC%11=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@H](CC(O)=O)N
Biological Activity: Jingzhaotoxin-III is a potent and selective blocker of Nav1.5 channels, with an IC50 of 348 nM, and shows no effect on other sodium channel isoforms. Jingzhaotoxin-III can selectively inhibit the activation of cardiac sodium channel but not neuronal subtypes, and hopefully represents an important ligand for discriminating cardiac VGSC subtype[1][2].
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Jingzhaotoxin-III | Jingzhaotoxin-III is a potent and selective blocker of Nav1.5 channels, with an IC50 of 348 nM, and shows no effect on other sodium channel isoforms. Jingzhaotoxin-III can selectively inhibit the activation of cardiac sodium channel but not neuronal subtypes, and hopefully represents an important ligand for discriminating cardiac VGSC subtype. | |||||||||||||||||||||
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References
- [1]. Rong M, et, al. Molecular basis of the tarantula toxin jingzhaotoxin-III (β-TRTX-Cj1α) interacting with voltage sensors in sodium channel subtype Nav1.5. FASEB J. 2011 Sep; 25(9): 3177-85. [Content Brief]
- [2]. Xiao Y, et, al. Jingzhaotoxin-III, a novel spider toxin inhibiting activation of voltage-gated sodium channel in rat cardiac myocytes. J Biol Chem. 2004 Jun 18; 279(25): 26220-6. [Content Brief]
