Tertiapin-LQ is a tertiapin-Q derivative that blocks Kir1.1 channels. It does so by binding to the external vestibule of the K+-conduction pore that is formed by the linker between the first and second transmembrane (M1-M2) segments.
产品描述
A Blocker of Kir1.1, Kir3.1 and Kir3.4 K+ Channels
产品形式
Inward-rectifier K+ (Kir) channels play many important biological roles and are emerging as important therapeutic targets. Tertiapin (TPN), a toxin present in honey bee venom (Apis mellifera) inhibits certain subtypes of inward-rectifier K+ channels. TPN is a highly compact peptide of 21 residues. Its C-terminal portion (histidine 12 to glycine 19) adopts an α-helical structure, whereas the N-terminal half acquires extended conformations. Two pairs of disulfide bonds help to hold the two parts together. Tertiapin inhibits ROMK1 (Kir1.1) and G-protein-gated channel (GIRK1/4) (Kir3.1/3.4) channels with IC50 values of 8.6 and 2.0 nM respectively and is selective over Kir2.1 channels. In accordance, it was shown to inhibit acetylcholine induced K+ currents in mammalian cardiomyocytes.
保存建议
艾美捷为您提供的Alonmone Labs原装进口的Tertiapin-LQ (5 x 1 mg)产品可室温运输，建议您在收到产品后将其置于合适的温度下保存。
