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Biological Data Biological description Potent and non-selective Kv 1.3 channel blocker (IC50 = approx. 30 pM; Kd = 11.7 pM). Also inhibits Kv 1.2 and Kv 1.1 channels (Kd values are 6.4 pM and 4.2 nM respectively). Blocks VEGF-induced Ca2+ entry and hyperpolarisation of endothelial cells.
Solubility & Handling Storage instructions -20°C
Solubility overview Soluble in water
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.
Chemical Data Molecular Formula C178 H286 N52 O50 S7
PubChem identifier 121596045
SMILES [H]N[C@@H]([C@@H](C)O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]4CCCN4C(=O)[C@H](CO)NC(=O)[C@@H](NC1=O)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC2=O)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC1=CNC=N1)C(O)=O
InChiKey OVJBOPBBHWOWJI-FYNXUGHNSA-N
References for Margatoxin References are publications that support the biological activity of the product
Margatoxin is a non-selective inhibitor of human Kv1.3 K+ channels. Bartok A et al (2014) Toxicon 87 : 6-16. Margatoxin inhibits VEGF-induced hyperpolarization, proliferation and nitric oxide production of human endothelial cells. Erdogan A et al (2005) J Vasc Res 42(5) : 368-76. Purification, characterization, and biosynthesis of margatoxin, a component of Centruroides margaritatus venom that selectively inhibits voltage-dependent potassium channels. Garcia-Calvo M et al (1993) J Biol Chem 268(25) : 18866-74.
Potent, non-selective Kv 1.3 channel blocker
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