ASIC3 selective inhibitor(酸敏感离子通道3 (ASIC3 )选择性抑制剂)

APETx2 is a toxin that was originally isolated from Anthopleura elegantissima (Sea anemone). selectively blocks the H(+)-gated sodium channel ASIC3 (ACCN3). The blockage is rapid and reversible. This toxin does not block isoform ASIC1a (unlike Psalmotoxin 1) and isoform ASIC1b of ASIC1 (ACCN2), nor ASIC2 (ACCN1). It also inhibits the heteromeric ASIC2b-ASIC3 channel, and has less affinity for ASIC1b-ASIC3, ASIC1a-ASIC3, and no effect on the ASIC2a-ASIC3 channels. IC₅₀ is 63 nM on ASIC3 channel. IC₅₀ is 117 nM on ASIC2b-ASIC3 heteromeric channel. IC₅₀ is 0.9 µM on ASIC1b-ASIC3 heteromeric channel. IC₅₀ is 2 µM on ASIC1a-ASIC3 heteromeric channel. Interestingly, recent studies demonstrated that also inhibits Na_v1.8 currents with an IC₅₀ of around 2 µM.

技术资料

氨基酸序列：

 H-Gly-Thr-Ala-Cys⁴-Ser-Cys⁶-Gly-Asn-Ser-Lys-Gly-Ile-Tyr-Trp-Phe-Tyr-Arg-Pro-Ser-Cys²⁰-Pro-Thr-Asp-Arg-Gly-Tyr-Thr-Gly-Ser-Cys³⁰-Arg-Tyr-Phe-Leu-Gly-Thr-Cys³⁷-Cys³⁸-Thr-Pro-Ala-Asp-OH

二硫键： Disulfide bonds between Cys⁴-Cys³⁷, Cys⁶-Cys³⁰ and Cys²⁰-Cys³⁸

长度 (aa)：42

分子式： C₁₉₆H₂₈₀N₅₄O₆₁S₆ 

分子量：  4561.13 Da

外观：White lyophilized solid 

可溶性： water and saline buffer

CAS 号： not available 

来源： Synthetic 

纯度： > 98%

产品信息