XE991

Applications
Specifications
Scientific Background

Overview

Cat #: X-100

Purity: >95%

CAS No.: 122955-42-4

MW: 376.45

Form: Lyophilized

XE991 (#X-100) is a highly pure, synthetic, and biologically active compound.

Certificate of Analysis SDS

Structure

For research purposes only, not for human use

Applications

Citations (2)

Citations

Product citations

Muqeem, T. et al. (2018) J. Neurosci. 38, 3729.
Nassoiy, S.P. et al. (2017) J. Biomed. Sci. 24, 8.

Specifications

Properties

Technical Specifications

MW 376.45

Purity >95%

Molecular formula C₂₆H₂₀N₂O.

Form Lyophilized powder.

CAS No. 122955-42-4

Source Synthetic

Chemical name 10,10-bis(4-Pyridinylmethyl)-9(10H)-anthracenone.

Biological Activity

Target KCNQ K⁺ channels

Effective concentration 0.1-300 µM.

References

Wang, H.S. et al. (2000) Mol. Pharmacol. 57, 1218.

Solubility and Storage

Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.

Solubility 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g 1 min).

Storage of solutions Up to four weeks at 4°C or three months at -20°C.

Scientific Background

Scientific background

Voltage-gated K⁺ channels of the KCNQ family (K_V7) are widely expressed in nerves and smooth muscles where their general role is to hyperpolarise the cell membrane and thereby dampen excitability¹.

XE991 is a potent and selective blocker of KCNQ voltage-gated K⁺ channels. It blocks K_V7.2 + K_V7.3 (KCNQ2 + KCNQ3)/M-currents (IC₅₀ = 0.6 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)¹. Suppression of the M-current causes an increase in intrinsic excitability². 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 therapeutics². It was demonstrated that XE991 enhances learning and memory in healthy mice³.