XE 991 dihydrochloride

Name: XE 991 dihydrochloride
Brand: Tocris Bioscience
SKU: 2000
Rating: 5 (1 reviews)

Catalog # 2000 | Tocris Bioscience a Bio-Techne Brand

(1)

Citations (34)

COA / SDS

Potent, selective KV7 (KCNQ) channel blocker; blocks M-currents

Key Product Details

Description:	Potent, selective K_V7 (KCNQ) channel blocker; blocks M-currents
Chemical Name:	10,10-bis(4-Pyridinylmethyl)-9(10H)-anthracenone dihydrochloride
Purity:	≥99% (HPLC)
Molecular Weight:	449.37

View Full Technical Details for XE 991 dihydrochloride

Technical Data
Citations (34) / Reviews (1)

Biological Activity for XE 991 dihydrochloride

XE 991 dihydrochloride is a 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 for XE 991 dihydrochloride

M. Wt	449.37
Formula	C₂₆H₂₀N₂O.2HCl
Storage	Desiccate at RT
Purity	≥99% (HPLC)
CAS Number	122955-13-9
PubChem ID	45073462
InChi Key	WOGWMARIFDNZON-UHFFFAOYSA-N
Smiles	Cl.Cl.O=C1C2=C(C=CC=C2)C(CC2=CC=NC=C2)(CC2=CC=NC=C2)C2=C1C=CC=C2

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.

Solubility for XE 991 dihydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	water	44.94	100

Preparing Stock Solutions for XE 991 dihydrochloride

The following data is based on the product molecular weight 449.37.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.23 mL	11.13 mL	22.25 mL
5 mM	0.45 mL	2.23 mL	4.45 mL
10 mM	0.22 mL	1.11 mL	2.23 mL
50 mM	0.04 mL	0.22 mL	0.45 mL

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References for XE 991 dihydrochloride

References are publications that support the biological activity of the product.

Passmore KCNQ/M currents in sensory neurons: significance for pain therapy. J.Neurosci. 2003 PMID: 12904483
Wang Molecular basis for differential sensitivity of KCNQ and I_Ks channels to the cognitive enhancer XE991. Mol.Pharmacol. 2000 PMID: 10825393
Wang KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel. Science 1998 PMID: 9836639
Zaczek 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. 1998 PMID: 9580619

Citations for XE 991 dihydrochloride (34)

Showing 1 - 10 of 34 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for XE 991 dihydrochloride include:

Pagani et al. (2019) How Gastrin-Releasing Peptide Opens the Spinal Gate for Itch. Neuron. 2019;
PMID: 31103358
Georgilis et al. (2018) PTBP1-Mediated Alternative Splicing Regulates the Inflammatory Secretome and the Pro-tumorigenic Effects of Senescent Cells. Cancer Cell. 34:85
PMID: 29990503
Greene et al. (2017) XE991 and Linopirdine are state-dependent inhibitors for Kv7/KCNQ channels that favor activated single subunits. J.Pharmacol.Exp.Ther.. 362:177
PMID: 28483800
Lezmy (2017) M-current inhibition rapidly induces a unique CK2-dependent plasticity of the axon initial segment. Proc Natl Acad Sci U S A. 114(47):E10234
PMID: 29109270
Salzer et al. (2016) Control of sensory neuron excitability by serotonin involves 5HT2C receptors and Ca2+-activated chloride channels. Neuropharmacology. 110 (A):277
PMID: 27511837
Bordas et al. (2015) The M-current contributes to high threshold membrane potential oscillations in a cell type-specific way in the pedunculopontine nucleus of mice. Mol Brain. 9:121
PMID: 25904846
Lee et al. (2015) N-MthD.-aspartate receptors mediate activity-dependent down-regulation of potassium channel genes during the expression of homeostatic intrinsic plasticity. J Neurosci. 8:4
PMID: 25599691
Sobieski et al. (2015) Loss of Local Astrocyte Support Disrupts Action Potential Propagation and Glutamate Release Synchrony from Unmyelinated Hippocampal Axon Terminals In Vitro. Front Behav Neurosci. 35:11105
PMID: 26245971
Parent et al. (2015) Cholinergic and ghrelinergic receptors and KCNQ channels in the medial PFC regulate the expression of palatability. Front Syst Neurosci. 9:284
PMID: 26578914
Meredith et al. (2015) Kv1 channels and neural processing in vestibular calyx afferents. Mol Pharmacol. 9:85
PMID: 26082693
Pérez-Ramírez et al. (2015) KV7 Channels Regulate Firing during Synaptic Integration in GABAergic Striatal Neurons. PLoS One. 2015:472676
PMID: 26113994
Robbins et al. (2013) Effects of KCNQ2 gene truncation on M-type Kv7 potassium currents. PLoS One. 8:e71809
PMID: 23977150
Ooi et al. (2013) Triple cysteine module within M-type K+ channels mediates reciprocal channel modulation by nitric oxide and reactive oxygen species. Neural Plast. 33:6041
PMID: 23554485
Boehlen et al. (2013) Contribution of near-threshold currents to intrinsic oscillatory activity in rat medial entorhinal cortex layer II stellate cells. J Neurophysiol. 109:445
PMID: 23076110
Rubi et al. (2013) Raised activity of L-type calcium channels renders neurons prone to form paroxysmal depolarization shifts. Neuromolecular Med. 15:476
PMID: 23695859
Leitner et al. (2012) Restoration of ion channel function in deafness-causing KCNQ4 mutants by synthetic channel openers. Br J Pharmacol. 165:2244
PMID: 21951272
Passmore et al. (2012) Functional significance of M-type potassium channels in nociceptive cutaneous sensory endings. Front Mol Neurosci. 5:63
PMID: 22593734
He et al. (2012) Increased Kv1 channel expression may contribute to decreased sIPSC frequency following chronic inhibition of NR2B-containing NMDAR. Neuropsychopharmacology. 37:1338
PMID: 22218089
Köhn et al. (2012) Differential effects of cystathionine-γ-lyase-dependent vasodilatory H2S in periadventitial vasoregulation of rat and mouse aortas. J Physiol. 7:e41951
PMID: 22870268
Zemkova et al. (2011) NE causes a biphasic change in mammalian pinealocye membrane potential: role of alpha1B-adrenoreceptors, phospholipase C, and Ca²⁺. Endocrinology. 152:3842
PMID: 21828176
Zhang et al. (2011) AKAP79/150 signal complexes in G-protein modulation of neuronal ion channels. J Neurosci. 31:7199
PMID: 21562284
Geier et al. (2011) Dynamic interplay of excitatory and inhibitory coupling modes of neuronal L-type calcium channels. Am J Physiol Cell Physiol. 300:C937
PMID: 21228322
McCallum et al. (2011) The contribution of Kv7 channels to pregnant mouse and human myometrial contractility. J Neurosci. 15:577
PMID: 20132415
Ipavec et al. (2011) KV7 channels regulate muscle tone and nonadrenergic noncholinergic relaxation of the rat gastric fundus. Pharmacol Res. 64:397
PMID: 21740972
Bi et al. (2011) Visceral hyperalgesia induced by forebrain-specific suppression of native Kv7/KCNQ/M-current in mice. Mol Pain. 7:84
PMID: 22029713
Xu et al. (2009) MinK-dependent internalization of the IKs potassium channel. Cardiovasc Res. 82:430
PMID: 19202166
Joshi et al. (2009) KCNQ modulators reveal a key role for KCNQ potassium channels in regulating the tone of rat pulmonary artery smooth muscle. J Neurosci. 329:368
PMID: 19151245
Anderson et al. (2009) KCNQ currents and their contribution to resting membrane potential and the excitability of interstitial cells of Cajal from the guinea pig bladder. J.Urol.. 182:330
PMID: 19450820
Kim and Marcus (2009) Endolymphatic sodium homeostasis by extramacular epithelium of the saccule. J Neurosci. 29:15851
PMID: 20016101
Kim et al. (2009) Regulation of ENaC-mediated sodium transport by glucocorticoids in Reissner's membrane epithelium. Am J Physiol Cell Physiol. 296:C544
PMID: 19144862
Linley et al. (2008) Inhibition of M current in sensory neurons by exogenous proteases: a signaling pathway mediating inflammatory nociception. Br J Pharmacol. 28:11240
PMID: 18971466
Wladyka et al. (2008) The KCNQ/M-current modulates arterial baroreceptor function at the sensory terminal in rats. J Pharmacol Exp Ther. 586:795
PMID: 18048450
Strøbaek et al. (2006) 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. J Cell Mol Med. 70:1771
PMID: 16926279
Yeung and Greenwood (2005) Electrophysiological and functional effects of the KCNQ channel blocker XE991 on murine portal vein smooth muscle cells. J Pharmacol Exp Ther. 146:585
PMID: 16056238

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XE 991 worked ideally in lab coditions, produced reproducible data

Name: Anonymous

Species: Mouse

Assay Type: In Vitro

XE 991 is a potent Kv7 channel blocker.My study focused on to finding out whether it shows the same blocking effect on Kv11.1 channels. The product worked ideally in lab coditions, produced reproducible data. Would purchase again.

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