CP 339818 hydrochloride is a potent KV1.3 channel antagonist that preferentially binds to the C-type inactivated state of the channel. It appears to recognize only the inactivated conformation of KV1.3. CP 339818 hydrochloride inhibits KV1.3 expressed in brain and in T lymphocyte cells with an IC50 value of ~ 200 nM. In addition to its effect on KV1.3, CP 339818 inhibits the Shaker-related A-type K+ channel, KV1.4, expressed in brain cells with an IC50 of ~ 300 nM. CP 339818 is significantly less potent blocker of KV1.1, KV1.2, KV1.5, KV1.6, KV3.1-4, and KV4.2. CP 339818 is valuable for immune system studies, where the absence of KV1.4 makes it functionally selective for KV1.3, and it has shown suppression of T cell activation. CP 339818 hydrochloride is also valuable for the study of KV1.4 function1.
产品描述
A Blocker of KV1.3 and KV1.4 K+ Channels
产品形式
CP 339818 hydrochloride is a potent KV1.3 channel antagonist that preferentially binds to the C-type inactivated state of the channel. It appears to recognize only the inactivated conformation of KV1.3. CP 339818 hydrochloride inhibits KV1.3 expressed in brain and in T lymphocyte cells with an IC50 value of ~ 200 nM. In addition to its effect on KV1.3, CP 339818 inhibits the Shaker-related A-type K+ channel, KV1.4, expressed in brain cells with an IC50 of ~ 300 nM. CP 339818 is significantly less potent blocker of KV1.1, KV1.2, KV1.5, KV1.6, KV3.1-4, and KV4.2. CP 339818 is valuable for immune system studies, where the absence of KV1.4 makes it functionally selective for KV1.3, and it has shown suppression of T cell activation. CP 339818 hydrochloride is also valuable for the study of KV1.4 function1.