- Alomone Labs Tertiapin inhibits Kir3.2 channels expressed in Xenopus oocytes.A continuous current trace recorded at a holding potential of -80 mV. Channel activation was achieved by high K+ solution perfusion. 50 nM Tertiapin (#STT-250) was applied during the period (2 minutes each) marked as a green trace.
Tertiapin is a 21 amino acid long toxin, originally isolated from Apis mellifera bee venom. Native and synthetic Tertiapin block a range of inward rectifier K+ channels. (Kir), in particular ROMK1 (Kir1.1, IC50 = 2 nM) and GIRK (Kir3 family, IC50 for the Kir3.1/3.4 heteromer is 8.6 nM) but with no effect on Kir2 family members1. In addition, it was shown to inhibit acetylcholine-induced K+ currents in the heart2,3.
Tertiapin is as active as Tertiapin-Q (#STT-170), a derivative of Tertiapin in which the oxidation-liable methionine is replaced by a glutamine residue4.
Tertiapin (#STT-250) is a highly pure, synthetic, and biologically active peptide toxin.