Name: XE991 dihydrochloride
Brand: Alomone Labs
SKU: X-101

Overview

Cat #: X-101

Lyophilized Powder yes

Source Synthetic

MW: 449.37

Purity: >98%

Form Lyophilized powder.

Effective concentration 0.1-300 µM.

Structure

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

Molecular formula C₂₆H₂₂Cl₂N₂O.

CAS No.: 122955-13-9

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

References-Activity

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

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.

Our bioassay

Alomone Labs XE991 dihydrochloride blocks KCNQ2/KCNQ3 channels heterologously expressed in Xenopus oocytes.
A. Time course of KCNQ2/KCNQ3 maximal current amplitude, elicited by 700 ms voltage step from holding potential of -100 mV to -30 mV, delivered every 10 seconds. Application of 100 µM XE991 dihydrochloride (#X-101) inhibits the KCNQ2/KCNQ3 current in a reversible manner (indicated by the horizontal bar). B. Representative current traces before and during application of 100µM XE991 dihydrocloride as indicated.

References - Scientific background

Yeung, S.Y. and Greenwood, I.A. (2005) Br J Pharmacol. 146, 585.
Zaczek, R. et al. (1998) Pharmacol. Exp. Ther. 285, 724.
Fontán-Lozano, A. et al. (2009) Hippocampus 21, 22.

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.

Target KCNQ K⁺ channels

Lyophilized Powder

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

Certificate of Analysis SDS

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

Last Update: 07/05/2024

Applications

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.

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XE991 dihydrochloride

Overview

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Citations

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Scientific Background

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