XE991

XE991 is a synthetic, potent, and selective blocker of KCNQ (Kv7) family voltage-gated potassium channels, particularly inhibiting KCNQ2/KCNQ3 (Kv7.2/Kv7.3) heteromers ("M-currents") and KCNQ1 (Kv7.1) homomers. It acts in a state-dependent manner by preferentially inhibiting activated (open) Kv7 channel subunits, with submicromolar inhibitory potency (IC50 ≈ 0.6–0.75 µM for KCNQ2/3 and KCNQ1). Blockade of these channels increases intrinsic excitability in neurons and smooth muscle, augments neurotransmitter release (such as acetylcholine), and has shown cognitive enhancing effects in animal models. XE991 is primarily used as a research tool to study the physiological and pathophysiological roles of M-currents in neuronal, muscular, and vascular tissue, with potential implications for central nervous system disorders such as Alzheimer’s disease and for vascular contractility research[1][2][3][5][9].

Other names

XE991 dihydrochlorideXE-991 dihydrochlorideXE 991 dihydrochloride