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Guangxitoxin 1E is a potent and selective blocker of K V 2.1 and K V 2.2 channels . Guangxitoxin 1E inhibits K V 2 with an IC 50 of 1-3 nM. K V 2 channels underlie delayed-rectifier potassium currents in various neurons
In Vitro
Guangxitoxin 1E inhibits K V 2 with an IC 50 of 1-3 nM but has no significant effect on K V 1.2, K V 1.3, K V 1.5, K V 3.2 and BK potassium channels, nor on calcium and sodium channels Ca V 1.2, Ca V 2.2, Na V 1.5, Na V 1.7, Na V 1.8, whereas the IC 50 for K V 4.3 channels is 24-54 nM. In mouse β-cells, Guangxitoxin 1E inhibits 90% of I DR and, as for K V 2.1, shifts the voltage dependence of channel activation to more depolarized potentials, a characteristic of gating-modifier peptides. Guangxitoxin 1E broadens theβ-cell action potential, enhances glucose-stimulated intracellular calcium oscillations, and enhances insulin secretion from mouse pancreatic islets in a glucose-dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:IC50: 1-3 nM (K V 2 channels),24-54 nM (K V 4.3 channels)