Guangxitoxin 1E 

Selective blocker of K_v2.1 and K_v2.2(鉀離子通道K_v2.1 和 K_v2.2選擇性阻斷劑)

Guangxitoxin-1E (GxTx-1E) was isolated from the venom of Chilobrachys jingzhao (Chinese earth tiger tarantula).Guangxitoxin-1E was shown to block K_v2.1/KCNB1, K_v2.2/KCNB2 and K_v4.3/KCND3 channels without significant effect on K_v1.2/KCNA2, K_v1.3/KCNA3, K_v1.5/KCNA5, K_v3.2/KCNC2, Ca_v1.2/CACNA1C, Ca_v2.2/CACNA1B, Na_v1.5/SCN5A, Na_v1.7/SCN9A or Na_v1.8/SCN10A channels. Guangxitoxin-1E inhibits K_v2.1 with an IC₅₀ value of 1 nM and K_v2.2 with an IC₅₀ value of 3 nM. Block of K_v4.3 occurs at 10-20 fold higher concentrations. Guangxitoxin-1E acts as a gating modifier since it shifts the voltage-dependence of K_v2.1 K⁺ currents towards depolarized potentials. In pancreatic beta-cells, Guangxitoxin-1E enhances glucose-stimulated insulin secretion by broadening the cell action potential and enhancing calcium oscillations.

治療領(lǐng)域：Diabetes type 2（II型糖尿病）

Guangxitoxin-1E 技術(shù)資料

氨基酸序列：

 Glu-Gly-Glu-Cys⁴-Gly-Gly-Phe-Trp-Trp-Lys-Cys¹¹-Gly-Ser-Gly-Lys-Pro-Ala-Cys¹⁸-Cys¹⁹-Pro-Lys-Tyr-Val-Cys²⁴-Ser-Pro-Lys-Trp-Gly-Leu-Cys³¹-Asn-Phe-Pro-Met-Pro-OH 

二硫鍵（Presumed disulfide bridge pattern）： Cys⁴-Cys¹⁹, Cys¹¹-Cys²⁴ and Cys¹⁸-Cys³¹ 

長度 (aa)：36 

分子式：C₁₇₈H₂₄₈N₄₄O₄₅S₇ 

分子量：3948.70 Da 

外觀：White lyophilized solid 

可溶性：water and saline buffer 

CAS 號：not available 

來源：Synthetic 

純度： > 95%

產(chǎn)品信息