UK-78282 hydrochloride is a novel piperidine blocker of the T lymphocyte voltage-gated K+ channel, KV1.3 and KV1.4 with IC50 values of 0.28 and 0.17 μM respectively. UK-78282 suppresses T lymphocyte mitogenesis and leads to membrane depolarization. UK-78282 also blocks KV1.4 expressed in heart and brain. UK-78282 preferentially blocks the C-type inactivated state of the KV1.3 channel. KV1.3 mutants containing hydrophobic residues that might prefer to be buried, transition slowly into the C-type inactivated conformation and are insensitive to block by UK-78282, possibly because of the inability of the drug to bind the channel. UK-78282 hydrochloride serves as an experimental tool to probe the conformational changes in KV1.3 leading to C-type inactivation and to further define the critical physiological role of KV1.3 in T lymphocyte activation.
产品描述
A Blocker of KV1.3 and KV1.4 K+ Channels
产品形式
UK-78282 hydrochloride is a novel piperidine blocker of the T lymphocyte voltage-gated K+ channel, KV1.3 and KV1.4 with IC50 values of 0.28 and 0.17 μM respectively. UK-78282 suppresses T lymphocyte mitogenesis and leads to membrane depolarization. UK-78282 also blocks KV1.4 expressed in heart and brain. UK-78282 preferentially blocks the C-type inactivated state of the KV1.3 channel. KV1.3 mutants containing hydrophobic residues that might prefer to be buried, transition slowly into the C-type inactivated conformation and are insensitive to block by UK-78282, possibly because of the inability of the drug to bind the channel. UK-78282 hydrochloride serves as an experimental tool to probe the conformational changes in KV1.3 leading to C-type inactivation and to further define the critical physiological role of KV1.3 in T lymphocyte activation.
