XE 991 dihydrochloride
Cat. No. 2000
Chemical Name: 10,10-bis(4-Pyridinylmethyl)-9(10H)
Biological ActivityPotent and selective blocker of KV7 (KCNQ) voltage-gated potassium channels. Blocks KV7.2+7.3 (KCNQ2+3) / M-currents (IC50 = 0.6 - 0.98 μM) and KV7.1 (KCNQ1) homomeric channels (IC50 = 0.75 μM) but is less potent against KV7.1/minK channels (IC50 = 11.1 μM). Augments hippocampal ACh release and is a cognitive enhancer following oral administration in vivo.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Safety Data Sheet
Wang et al (1998) KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel. Science 282 1890. PMID: 9836639.
Zaczek et al (1998) Two new potent neurotransmitter release enhancers, 10,10-bis(4-pyridinylmethyl)-9(10H)-anthracenone and 10,10-bis(2-fluoro-4-pyridinylmethyl)-9(10H)-anthracenone: comparison to linopirdine. J.Pharmacol.Exp.Ther. 285 724. PMID: 9580619.
Wang et al (2000) Molecular basis for differential sensitivity of KCNQ and IKs channels to the cognitive enhancer XE991. Mol.Pharmacol. 57 1218. PMID: 10825393.
Passmore et al (2003) KCNQ/M currents in sensory neurons: significance for pain therapy. J.Neurosci. 23 7227. PMID: 12904483.
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Keywords: XE 991 dihydrochloride, supplier, KCNQ, channel, blockers, Potassium, KV, Channels, voltage-gated, voltage-dependent, K+, KCNQ2, KCNQ3, KCNQ1, XE991, dihydrochloride, KV7.1
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