XE991 is a potent and selective blocker of KV7 (KCNQ) voltage-gated K+ channels. It Blocks KV7.2+ KV7.3 (KCNQ2+ KCNQ3)/M-currents (IC50 = 0.6 μM) and KV7.1 (KCNQ1) homomeric channels (IC50 = 0.75 μM) but is less potent against KV7.1/minK channels (IC50 = 11.1 μM). Suppression of the M-current causes an increase in intrinsic excitability. XE991 enhances acetylcholine release from rat brain slices (EC50 = 490 nM) and shows good in vivo potency and duration of action, suggesting utility in Alzheimer’s disease therapeutics. It was demonstrated that XE991 enhances learning and memory in healthy mice.
产品描述
A Blocker of KV7 K+ Channels
产品形式
Voltage-gated K+ channels of the KCNQ family (KV7) are widely expressed in nerves and smooth muscles where their general role is to hyperpolarise the cell membrane and thereby dampen excitability.