产品
编 号：F084529
分子式：C178H248N44O45S7
分子量：3948.61
分子式：C178H248N44O45S7
分子量：3948.61
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CAS No: 1233152-82-3
产品详情
生物活性：
Guangxitoxin 1E is a potent and selective blocker of KV2.1 and KV2.2 channels. Guangxitoxin 1E inhibits KV2 with an IC50 of 1-3 nM. KV2 channels underlie delayed-rectifier potassium currents in various neurons.
体外研究：
Guangxitoxin 1E inhibits KV2 with an IC50 of 1-3 nM but has no significant effect on KV1.2, KV1.3, KV1.5, KV3.2 and BK potassium channels, nor on calcium and sodium channels CaV1.2, CaV2.2, NaV1.5, NaV1.7, NaV1.8, whereas the IC50 for KV4.3 channels is 24-54 nM.In mouse β-cells, Guangxitoxin 1E inhibits 90% of IDR and, as for KV2.1, 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.
Guangxitoxin 1E is a potent and selective blocker of KV2.1 and KV2.2 channels. Guangxitoxin 1E inhibits KV2 with an IC50 of 1-3 nM. KV2 channels underlie delayed-rectifier potassium currents in various neurons.
体外研究：
Guangxitoxin 1E inhibits KV2 with an IC50 of 1-3 nM but has no significant effect on KV1.2, KV1.3, KV1.5, KV3.2 and BK potassium channels, nor on calcium and sodium channels CaV1.2, CaV2.2, NaV1.5, NaV1.7, NaV1.8, whereas the IC50 for KV4.3 channels is 24-54 nM.In mouse β-cells, Guangxitoxin 1E inhibits 90% of IDR and, as for KV2.1, 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.
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