Potent, Non-peptide Kv1.3 and Kv1.4 Channel Blocker

CP 339818 is a novel, potent and selective non-peptide blocker of the Kv1.3 potassium channel. This compound inhibits Kv1.3 in a use-dependent manner by preferentially blocking the C-type inactivated state of the channel (IC₅₀ ~ 200 nM), as measured in T lymphocytes. In addition to its effect on Kv1.3, CP 339818 also inhibits the Shaker-related A-type K⁺ channel, Kv1.4 (IC₅₀ ~ 300 nM) and is one of the most potent known blockers of this channel. CP 339818 is selective over a range of other potassium channels, and the IC₅₀ values are shown in the table below.

The potency and selectivity of this non-peptide channel blocker make CP 339818 a highly useful experimental tool for studying Kv1.3 and Kv1.4.