XE991 dihydrochloride

Applications
Specifications
Scientific Background

Overview

Cat #: X-101

Purity: >98%

CAS No.: 122955-13-9

MW: 449.37

Form: Lyophilized

XE991 dihydrochloride (#X-101) is a highly pure, synthetic, and biologically active compound.

Certificate of Analysis SDS

Structure

Image & Title

Alomone Labs XE991 dihydrochloride inhibits KCNQ currents in mouse dorsal raphe nucleus neurons.Sample time course shows that KCNQ currents are completely blocked by 3 µM XE991 dihydrochloride (#X-101).Adapted from Zhao, C. et al. (2017) Front. Cell. Neurosci. 11, 405. with permission of Frontiers.

For research purposes only, not for human use

Applications

Citations (7)

Citations

Product citations

Inagaki, A. et al. (2019) Pflugers Arch. 471, 313.
Li, L. et al. (2017) Br. J. Pharmacol. 174, 4277.
Zhao, C. et al. (2017) Front. Cell. Neurosci. 11, 405.

Specifications

Properties

Technical Specifications

MW 449.37

Purity >98%

Molecular formula C₂₆H₂₂Cl₂N₂O.

Form Lyophilized powder.

CAS No. 122955-13-9

Source Synthetic

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

Biological Activity

Target KCNQ K⁺ channels

Effective concentration 0.1-300 µM.

Activity XE991 blocks KCNQ channels with IC₅₀ of 0.5-10 µM¹.

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 Up to 50mM in water. Mild warming or agitation may be required. Spin-down all product preparations before handling.

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.