Kv1.3 selective blocker

Margatoxin (MgTx) is a component of the venom of Scorpio Centruroides margaritatus. Margatoxin 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.

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AA sequence: Thr-Ile-Ile-Asn-Val-Lys-Cys7-Thr-Ser-Pro-Lys-Gln-Cys13-Leu-Pro-Pro-Cys17-Lys-Ala-Gln-Phe-Gly-Gln-Ser-Ala-Gly-Ala-Lys-Cys29-Met-Asn-Gly-Lys-Cys34-Lys-Cys36-Tyr-Pro-His-OH
(Disulfide bonds between Cys7-Cys29, Cys13-Cys34 and Cys17-Cys36)
Length (aa): 39
Formula: C178H286N52O50S7
Molecular Weight: 4179.03 Da
Appearance: White lyophilized solid
Solubility: water and saline buffer
CAS number: [145808-47-5] Source: Synthetic
Purity rate: > 97 %


Potent suppression of vascular smooth muscle cell migration and human neointimal hyperplasia by KV1.3 channel blockers

Kv1.3 channels in postganglionic sympathetic neurons: expression, function, and modulation

Potent suppression of Kv1.3 potassium channel and IL-2 secretion by diphenyl phosphine oxide-1 in human T cells

The effects of Kv1.3 and IKCa1 potassium channel inhibition on calcium influx of human peripheral T lymphocytes in rheumatoid arthritis

Overexpression of Delayed Rectifier K(+) Channels Promotes In situ Proliferation of Leukocytes in Rat Kidneys with Advanced Chronic Renal Failure

Characteristics of ACh-induced hyperpolarization and relaxation in rabbit jugular vein

Charybdotoxin and margatoxin acting on the human voltage-gated potassium channel hKv1.3 and its H399N mutant: an experimental and computational comparison

Voltage-dependent biphasic effects of chloroquine on delayed rectifier K(+)-channel currents in murine thymocytes

Different potassium channels are involved in relaxation of rat renal artery induced by P1075

Chemical synthesis and structure-function studies of margatoxin, a potent inhibitor of voltage-dependent potassium channel in human T lymphocytes

Determination of the three-dimensional structure of margatoxin by 1H, 13C, 15N triple-resonance nuclear magnetic resonance spectroscopy

Purification, characterization, and biosynthesis of margatoxin, a component of Centruroides margaritatus venom that selectively inhibits voltage-dependent potassium channels