IC50: 0.2 μM (KV2.1), 0.41 μM (KV2.2), 12.1 μM (KV1.2), 9.5 μM (KV1.5), >20 μM (KV3.2), 2.9 μM (KV11.1), 6.6 μM (CaV1.2), >10 μM (CaV2.1), >10 μM (CaV2.2), 5.7 μM (CaV2.3), >10 μM (NaV1.5), 8 μM (NaV1.7)[1]
KV2 channel inhibitor-1 is a selective KV2 channel inhibitor with IC50s of 0.2 μM and 0.41 μM for KV2.1 and KV2.2, respectively. KV2 channel inhibitor-1 possesses good selectivity over KV1.2 (IC50>10 μM). KV2 channel inhibitor-1 is >10-fold selective over NaV channels and other KV channels and displays weak activity on CaV channels[1].
KV2 channel inhibitor-1 (compound A1; 0.3, 1, 3 μM; 0-3000s) 抑制大鼠胰岛素瘤 INS-1 细胞中的 KV 电流。KV2 channel inhibitor-1 在 0.3 μM 时平均阻断 INS-1 KV 电流 71%，在 3 μM 时平均阻断 84%[1]。
[1]. James Herrington, et al. Identification of novel and selective Kv2 channel inhibitors. Mol Pharmacol. 2011 Dec;80(6):959-64.