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XE 991 dihydrochloride

Cat. No. 2000

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Chemical Name: 10,10-bis(4-Pyridinylmethyl)-9(10H)-anthracenone dihydrochloride

Biological Activity

Potent and selective blocker of K_V7 (KCNQ) voltage-gated potassium channels. Blocks K_V7.2+7.3 (KCNQ2+3) / M-currents (IC₅₀ = 0.6 - 0.98 μM) and K_V7.1 (KCNQ1) homomeric channels (IC₅₀ = 0.75 μM) but is less potent against K_V7.1/minK channels (IC₅₀ = 11.1 μM). Augments hippocampal ACh release and is a cognitive enhancer following oral administration in vivo.

Technical Data

M.Wt:

449.37

Formula:

C₂₆H₂₀N₂O.2HCl

Solubility:

Soluble to 100 mM in water

Purity:

>99 %

Storage:

Desiccate at RT

CAS No:

122955-42-4

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

References

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 I_Ks 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