Uses
RPR-260243, a potent activator of human ether-a-go-go-related gene (hERG), slows deactivation and attenuates inactivation of hERG1 channels. RPR260243-modified HERG currents are inhibited by Dofetilide (IC50=58 nM). RPR260243 displays no activator-like effects on other voltage-dependent ion channels, including the closely related ERG3 K+ channel[1][2]. RPR-260243 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
References
[1] Wu W, et al. Concatenated hERG1 tetramers reveal stoichiometry of altered channel gating by RPR-260243. Mol Pharmacol. 2015;87(3):401-409. DOI:
10.1124/mol.114.096693[2] Kang J, et al. Discovery of a small molecule activator of the human ether-a-go-go-related gene (HERG) cardiac K+ channel. Mol Pharmacol. 2005;67(3):827-836. DOI:
10.1124/mol.104.006577
