Home / Voltage-gated Potassium Channel Blockers / XE 991 dihydrochloride

XE 991 dihydrochloride

Catalog #: 2000
35 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
2000/10
2000/50
XE 991 dihydrochloride | CAS No. 122955-13-9 | Voltage-gated Potassium Channel Blockers
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Description: Potent, selective KV7 (KCNQ) channel blocker; blocks M-currents

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

Purity: ≥99%

Product Details
Citations (35)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

XE 991 dihydrochloride is a potent 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.

Technical Data

M.Wt:
449.37
Formula:
C26H20N2O.2HCl
Solubility:
Soluble to 100 mM in water
Purity:
≥99%
Storage:
Desiccate at RT
CAS No:
122955-13-9

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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Citations for XE 991 dihydrochloride

The citations listed below are publications that use Tocris products. Selected citations for XE 991 dihydrochloride include:

35 Citations: Showing 1 - 10

  1. Lucanthone, a potential PPT1 inhibitor, perturbs stemness, reduces tumor microtube formation and slows the growth of temozolomide-resistant gliomas in vivo.
    Authors: Radin Et al.
    J.Pharmacol.Exp.Ther.  2024;
  2. How Gastrin-Releasing Peptide Opens the Spinal Gate for Itch.
    Authors: Pagani Et al.
    Neuron  2019;
  3. PTBP1-Mediated Alternative Splicing Regulates the Inflammatory Secretome and the Pro-tumorigenic Effects of Senescent Cells.
    Authors: Georgilis Et al.
    Cancer Cell  2018;34:85
  4. XE991 and Linopirdine are state-dependent inhibitors for Kv7/KCNQ channels that favor activated single subunits.
    Authors: Greene Et al.
    J.Pharmacol.Exp.Ther.  2017;362:177
  5. M-current inhibition rapidly induces a unique CK2-dependent plasticity of the axon initial segment.
    Authors: Lezmy
    Proc Natl Acad Sci U S A  2017;114(47):E10234
  6. Control of sensory neuron excitability by serotonin involves 5HT2C receptors and Ca2+-activated chloride channels.
    Authors: Salzer Et al.
    Neuropharmacology  2016;110 (A):277
  7. Kv1 channels and neural processing in vestibular calyx afferents.
    Authors: Meredith Et al.
    Mol Pharmacol  2015;9:85
  8. Cholinergic and ghrelinergic receptors and KCNQ channels in the medial PFC regulate the expression of palatability.
    Authors: Parent Et al.
    Front Syst Neurosci  2015;9:284
  9. The M-current contributes to high threshold membrane potential oscillations in a cell type-specific way in the pedunculopontine nucleus of mice.
    Authors: Bordas Et al.
    Mol Brain  2015;9:121
  10. N-MthD.-aspartate receptors mediate activity-dependent down-regulation of potassium channel genes during the expression of homeostatic intrinsic plasticity.
    Authors: Lee Et al.
    J Neurosci  2015;8:4
  11. Loss of Local Astrocyte Support Disrupts Action Potential Propagation and Glutamate Release Synchrony from Unmyelinated Hippocampal Axon Terminals In Vitro.
    Authors: Sobieski Et al.
    Front Behav Neurosci  2015;35:11105
  12. KV7 Channels Regulate Firing during Synaptic Integration in GABAergic Striatal Neurons.
    Authors: Pérez-Ramírez Et al.
    PLoS One  2015;2015:472676
  13. Effects of KCNQ2 gene truncation on M-type Kv7 potassium currents.
    Authors: Robbins Et al.
    PLoS One  2013;8:e71809
  14. Triple cysteine module within M-type K+ channels mediates reciprocal channel modulation by nitric oxide and reactive oxygen species.
    Authors: Ooi Et al.
    Neural Plast  2013;33:6041
  15. Raised activity of L-type calcium channels renders neurons prone to form paroxysmal depolarization shifts.
    Authors: Rubi Et al.
    Neuromolecular Med  2013;15:476
  16. Contribution of near-threshold currents to intrinsic oscillatory activity in rat medial entorhinal cortex layer II stellate cells.
    Authors: Boehlen Et al.
    J Neurophysiol  2013;109:445
  17. Differential effects of cystathionine-γ-lyase-dependent vasodilatory H2S in periadventitial vasoregulation of rat and mouse aortas.
    Authors: Köhn Et al.
    J Physiol  2012;7:e41951
  18. Functional significance of M-type potassium channels in nociceptive cutaneous sensory endings.
    Authors: Passmore Et al.
    Front Mol Neurosci  2012;5:63
  19. Increased Kv1 channel expression may contribute to decreased sIPSC frequency following chronic inhibition of NR2B-containing NMDAR.
    Authors: He Et al.
    Neuropsychopharmacology  2012;37:1338
  20. Restoration of ion channel function in deafness-causing KCNQ4 mutants by synthetic channel openers.
    Authors: Leitner Et al.
    Br J Pharmacol  2012;165:2244
  21. Visceral hyperalgesia induced by forebrain-specific suppression of native Kv7/KCNQ/M-current in mice.
    Authors: Bi Et al.
    Mol Pain  2011;7:84
  22. KV7 channels regulate muscle tone and nonadrenergic noncholinergic relaxation of the rat gastric fundus.
    Authors: Ipavec Et al.
    Pharmacol Res  2011;64:397
  23. AKAP79/150 signal complexes in G-protein modulation of neuronal ion channels.
    Authors: Zhang Et al.
    J Neurosci  2011;31:7199
  24. Dynamic interplay of excitatory and inhibitory coupling modes of neuronal L-type calcium channels.
    Authors: Geier Et al.
    Am J Physiol Cell Physiol  2011;300:C937
  25. The contribution of Kv7 channels to pregnant mouse and human myometrial contractility.
    Authors: McCallum Et al.
    J Neurosci  2011;15:577
  26. NE causes a biphasic change in mammalian pinealocye membrane potential: role of alpha1B-adrenoreceptors, phospholipase C, and Ca2+.
    Authors: Zemkova Et al.
    Endocrinology  2011;152:3842
  27. MinK-dependent internalization of the IKs potassium channel.
    Authors: Xu Et al.
    Cardiovasc Res  2009;82:430
  28. KCNQ modulators reveal a key role for KCNQ potassium channels in regulating the tone of rat pulmonary artery smooth muscle.
    Authors: Joshi Et al.
    J Neurosci  2009;329:368
  29. Endolymphatic sodium homeostasis by extramacular epithelium of the saccule.
    Authors: Kim and Marcus
    J Neurosci  2009;29:15851
  30. Regulation of ENaC-mediated sodium transport by glucocorticoids in Reissner's membrane epithelium.
    Authors: Kim Et al.
    Am J Physiol Cell Physiol  2009;296:C544
  31. KCNQ currents and their contribution to resting membrane potential and the excitability of interstitial cells of Cajal from the guinea pig bladder.
    Authors: Anderson Et al.
    J.Urol.  2009;182:330
  32. The KCNQ/M-current modulates arterial baroreceptor function at the sensory terminal in rats.
    Authors: Wladyka Et al.
    J Pharmacol Exp Ther  2008;586:795
  33. Inhibition of M current in sensory neurons by exogenous proteases: a signaling pathway mediating inflammatory nociception.
    Authors: Linley Et al.
    Br J Pharmacol  2008;28:11240
  34. Inhibitory gating modulation of small conductance Ca2+-activated K+ channels by the synthetic compound (R)-N-(benzimidazol-2-yl)-1,2,3,4-tetrahydro-1-naphtylamine (NS8593) reduces afterhyperpolarizing current in hippocampal CA1 neurons.
    Authors: Strøbaek Et al.
    J Cell Mol Med  2006;70:1771
  35. Electrophysiological and functional effects of the KCNQ channel blocker XE991 on murine portal vein smooth muscle cells.
    Authors: Yeung and Greenwood
    J Pharmacol Exp Ther  2005;146:585

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