Guangxitoxin-1E is a 36 amino acid peptidyl toxin isolated from the Chilobrachys jingzhao (Chinese earth tiger) tarantula venom and belongs to the huwentoxin-1 family. Guangxitoxin-1E is a gating modifier of Kv2.1 (KCNB1, IC50 of 1 nM), Kv2.2 (KCNB2, IC50 of 3 nM) and Kv4.3 (KCND3, IC50 of 50 nM) channels. In pancreatic b cells, it enhances glucose-stimulated insulin secretion by broadening the cell action potential and enhancing calcium oscillations. The physiological modulation of Kv2.1 channels during glucose-induced insulin secretion is MgATP-mediated3,4. No significant effect was found on Kv1.2 (KCNA2), Kv1.3 (KCNA3), Kv1.5 (KCNA5), Kv3.2 (KCNC2), Cav1.2 (CACNA1C), Cav2.2 (CACNA1B), Nav1.5 (SCN5A), Nav1.7 (SCN9A) or Nav1.8 (SCN10A) channels.
产品描述
A Potent Gating Modifier of KV2.1, KV2.2 and KV4.3 K+ Channels
产品形式
Guangxitoxin-1E is a 36 amino acid peptidyl toxin isolated from the Chilobrachys jingzhao (Chinese earth tiger) tarantula venom and belongs to the huwentoxin-1 family. Guangxitoxin-1E is a gating modifier of Kv2.1 (KCNB1, IC50 of 1 nM), Kv2.2 (KCNB2, IC50 of 3 nM) and Kv4.3 (KCND3, IC50 of 50 nM) channels. In pancreatic b cells, it enhances glucose-stimulated insulin secretion by broadening the cell action potential and enhancing calcium oscillations. The physiological modulation of Kv2.1 channels during glucose-induced insulin secretion is MgATP-mediated3,4. No significant effect was found on Kv1.2 (KCNA2), Kv1.3 (KCNA3), Kv1.5 (KCNA5), Kv3.2 (KCNC2), Cav1.2 (CACNA1C), Cav2.2 (CACNA1B), Nav1.5 (SCN5A), Nav1.7 (SCN9A) or Nav1.8 (SCN10A) channels.