L8230-100UG - MARGATOXIN
(Syn. : MgTx, Potassium channel toxin alpha-KTx 2.2)
Product ID |
L8230-100UG |
Name |
MARGATOXIN |
Molecular formula |
C178H286N52O50S7 |
Description |
A 39 amino-acids peptide with 3 disulfide bridges
, synthetic, initially isolated from the venom of the Central American bark scorpion Centruroides margaritatus.
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Biological activity |
MgTx preferentially inhibits voltage-dependent potassium channels Kv1.3 with an IC50 value around 50 pM (20 fold more potent than Charybdotoxin) and irreversibly inhibits the proliferation response of human T-cells at 20 µM concentration. Margatoxin is known to be less potent on Kv1.3 expressed in Xenopus Oocytes (IC50 around 1 nM). Margatoxin was also described to be a potent inhibitor of human vascular smooth muscle cell migration with an IC50 of 85 pM. |
| Safety Data Sheet Available on request, please Contact us Ref. SDS_L8230-100UG : unit price : free of charge |
Product code |
L8230-100UG |
Molecular weight |
4179.03 Da |
Product name |
MARGATOXIN |
Physical form |
White lyophilized solid |
CAS No. |
145808-47-5 |
Melting point |
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RTECS |
NA |
Solubility |
water and saline buffer |
UNIPROT |
P40755 |
Optical Activity |
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PubChem SID |
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PubChem CID |
90488858 |
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Purity |
> 98 % |
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Toxicity(LD50) |
No Data |
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Chemical Name |
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Storage & Reconstitution Recommandations |
Stable at room temperature, store preferably at 4°C
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Savety Recommandations |
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Product code |
L8230-100UG |
Product name |
MARGATOXIN |
- 1. Bednarek, M. A., et al. (1994) Chemical synthesis and structure-function studies of margatoxin, a potent inhibitor of voltage-dependent potassium channel in human T lymphocytes, Biochem Biophys Res Commun. ;
2. Cheong A., et al. (2011) Potent suppression of vascular smooth muscle cell migration and human neointimal hyperplasia by KV1.3 channel blockers. Cardiovasc Res. PMID 20884640 ;
3. Doczi MA. et al. (2008) Kv1.3 channels in postganglionic sympathetic neurons: expression, function, and modulation. Am J Physiol Regul Integr Comp Physiol. PMID 18614767 ;
4. Garcia-Calvo, et al. (1993) Purification, characterization, and biosynthesis of margatoxin, a component of Centruroides margaritatus venom that selectively inhibits voltage-dependent potassium channels, J Biol Chem. ;
5. Itoh T. et al. (2012) Characteristics of ACh-induced hyperpolarization and relaxation in rabbit jugular vein. Br J Pharmacol. PMID 22595036 ;
6. Johnson, B. A., et al. (1994) Determination of the three-dimensional structure of margatoxin by 1H, 13C, 15N triple-resonance nuclear magnetic resonance spectroscopy, Biochemistry. ;
7. Kazama I. et al. (2012) Voltage-dependent biphasic effects of chloroquine on delayed rectifier K(+)-channel currents in murine thymocytes. J Physiol Sci. PMID 22328488 ;
8. Kazama I., et al. (2012) Overexpression of Delayed Rectifier K(+) Channels Promotes In situ Proliferation of Leukocytes in Rat Kidneys with Advanced Chronic Renal Failure. Int J Nephrol. PMID 22701172 ;
9. Nikouee A. et al. (2012) Charybdotoxin and margatoxin acting on the human voltage-gated potassium channel hKv1.3 and its H399N mutant: an experimental and computational comparison. J Phys Chem B. ;
10. Novakovic A., et al. (2012) Different potassium channels are involved in relaxation of rat renal artery induced by P1075. Basic Clin Pharmacol Toxicol. ;
11. Toldi G., et al. (2013) The effects of Kv1.3 and IKCa1 potassium channel inhibition on calcium influx of human peripheral T lymphocytes in rheumatoid arthritis. Immunobiology. ;
12. Zhao N., et al. (2013) Potent suppression of Kv1.3 potassium channel and IL-2 secretion by diphenyl phosphine oxide-1 in human T cells. PLoS One.