Uses
CP-339818 is a non-peptide drug with potent Kv1.3 channel blocking activity. CP-339818 is able to effectively inhibit the activation of human T cells. By selectively blocking Kv1.3, CP-339818 is of great value in immune system research. The drug inhibits the C-type inactivated state of Kv1.3 channels in a use-dependent manner. CP-339818 has significantly weaker blocking effects on Kv1.1, Kv1.2, Kv1.5, Kv1.6, Kv3.1-4, and Kv4.2 channels, and only shows some inhibition on the Kv1.4 channel[1].
Biological Activity
Potent, non-peptide K V 1.3 channel antagonist that preferentially binds to the C-type inactivated state of the channel (IC 50 ~ 200 nM) . Inhibits K V 1.4 with an IC 50 of ~ 300 nM. Selective over K V 1.1, K V 1.2, K V 1.5, K V 1.6, K V 3.1-4, and K V 4.2.
References
[1] Novel nonpeptide agents potently block the C-type inactivated conformation of Kv1.3 and suppress T cell activation PMID:8967992
