CP-339818 is a potent, selective, non-peptide KV1.3 channel antagonist with IC50 of 200 nM.
CP-339818 displays selectivity over Kv1.1, Kv1.2, Kv1.5, Kv1.6, Kv3.1-4, and Kv4.2, with only exception Kv1.4 (IC50=300 nM), also has no effect on T cell channels (I(CRAC) and intermediate-conductance K(Ca)).
CP-339818 inhibits Kv1.3 in a use-dependent manner by preferentially blocking the C-type inactivated state of the channel; suppresses human T cell activation.
