XE991 | Alomone Labs X-100 product information

product summary

company name :

Alomone Labs

product type :

chemical

product name :

XE991

catalog :

X-100

more info or order :

Alomone Labs product webpage

citations: 36

Reference
Salehi M, Neumann I, Jurek B, Pandamooz S. Co-Stimulation of Oxytocin and Arginine-Vasopressin Receptors Affect Hypothalamic Neurospheroid Size. Int J Mol Sci. 2021;22: pubmed publisher
Vallejo Gracia A, Sastre D, Colomer Molera M, Sole L, Navarro Pérez M, Capera J, et al. KCNE4-dependent functional consequences of Kv1.3-related leukocyte physiology. Sci Rep. 2021;11:14632 pubmed publisher
Simkin D, Marshall K, Vanoye C, Desai R, Bustos B, Piyevsky B, et al. Dyshomeostatic modulation of Ca2+-activated K+ channels in a human neuronal model of KCNQ2 encephalopathy. elife. 2021;10: pubmed publisher
Park M, Choi B, Kho A, Lee S, Hong D, Jeong J, et al. Effects of Transient Receptor Potential Cation 5 (TRPC5) Inhibitor, NU6027, on Hippocampal Neuronal Death after Traumatic Brain Injury. Int J Mol Sci. 2020;21: pubmed publisher
Kamata Y, Kambe T, Chiba T, Yamamoto K, Kawakami K, Abe K, et al. Paclitaxel Induces Upregulation of Transient Receptor Potential Vanilloid 1 Expression in the Rat Spinal Cord. Int J Mol Sci. 2020;21: pubmed publisher
Su M, Li L, Wang J, Sun H, Zhang L, Zhao C, et al. Kv7.4 Channel Contribute to Projection-Specific Auto-Inhibition of Dopamine Neurons in the Ventral Tegmental Area. Front Cell Neurosci. 2019;13:557 pubmed publisher
Crabbé M, Van der Perren A, Bollaerts I, Kounelis S, Baekelandt V, Bormans G, et al. Increased P2X7 Receptor Binding Is Associated With Neuroinflammation in Acute but Not Chronic Rodent Models for Parkinson's Disease. Front Neurosci. 2019;13:799 pubmed publisher
Ray S, Salzer I, Kronschläger M, Boehm S. The paracetamol metabolite N-acetylp-benzoquinone imine reduces excitability in first- and second-order neurons of the pain pathway through actions on KV7 channels. Pain. 2019;160:954-964 pubmed publisher
Zhang Y, Reynolds J, Cragg S. Pauses in Cholinergic Interneuron Activity Are Driven by Excitatory Input and Delayed Rectification, with Dopamine Modulation. Neuron. 2018;98:918-925.e3 pubmed publisher
Chimote A, Balajthy A, Arnold M, Newton H, Hajdu P, Qualtieri J, et al. A defect in KCa3.1 channel activity limits the ability of CD8+ T cells from cancer patients to infiltrate an adenosine-rich microenvironment. Sci Signal. 2018;11: pubmed publisher
Muqeem T, Ghosh B, Pinto V, Lepore A, Covarrubias M. Regulation of Nociceptive Glutamatergic Signaling by Presynaptic Kv3.4 Channels in the Rat Spinal Dorsal Horn. J Neurosci. 2018;38:3729-3740 pubmed publisher
Hu W, Bean B. Differential Control of Axonal and Somatic Resting Potential by Voltage-Dependent Conductances in Cortical Layer 5 Pyramidal Neurons. Neuron. 2018;97:1315-1326.e3 pubmed publisher
Lam D, Momeni Z, Theaker M, Jagadeeshan S, Yamamoto Y, Ianowski J, et al. RAGE-dependent potentiation of TRPV1 currents in sensory neurons exposed to high glucose. PLoS ONE. 2018;13:e0193312 pubmed publisher
Chen W, Chi Y, Kang X, Liu Q, Zhang H, Li Z, et al. Accumulation of Cav3.2 T-type Calcium Channels in the Uninjured Sural Nerve Contributes to Neuropathic Pain in Rats with Spared Nerve Injury. Front Mol Neurosci. 2018;11:24 pubmed publisher
Benedetto R, Ousingsawat J, Wanitchakool P, Zhang Y, Holtzman M, Amaral M, et al. Epithelial Chloride Transport by CFTR Requires TMEM16A. Sci Rep. 2017;7:12397 pubmed publisher
Kuo Y, Tsao C. Neuroprotection against apoptosis of SK-N-MC cells using RMP-7- and lactoferrin-grafted liposomes carrying quercetin. Int J Nanomedicine. 2017;12:2857-2869 pubmed publisher
Vera J, Alcayaga J, Sanhueza M. Competition between Persistent Na+ and Muscarine-Sensitive K+ Currents Shapes Perithreshold Resonance and Spike Tuning in CA1 Pyramidal Neurons. Front Cell Neurosci. 2017;11:61 pubmed publisher
Weber L, Al Refae K, Ebbert J, Jagers P, Altmuller J, Becker C, et al. Activation of odorant receptor in colorectal cancer cells leads to inhibition of cell proliferation and apoptosis. PLoS ONE. 2017;12:e0172491 pubmed publisher
Nassoiy S, Byron K, Majetschak M. Kv7 voltage-activated potassium channel inhibitors reduce fluid resuscitation requirements after hemorrhagic shock in rats. J Biomed Sci. 2017;24:8 pubmed publisher
Yang T, Zhang H, Liang Q, Shi Y, Mei Y, Barrett P, et al. Small-Conductance Ca2+-Activated Potassium Channels Negatively Regulate Aldosterone Secretion in Human Adrenocortical Cells. Hypertension. 2016;68:785-95 pubmed publisher
Yamamoto K, Chiba N, Chiba T, Kambe T, Abe K, Kawakami K, et al. Transient receptor potential ankyrin 1 that is induced in dorsal root ganglion neurons contributes to acute cold hypersensitivity after oxaliplatin administration. Mol Pain. 2015;11:69 pubmed publisher
Hipólito L, Fakira A, Cabañero D, Blandón R, Carlton S, Morón J, et al. In vivo activation of the SK channel in the spinal cord reduces the NMDA receptor antagonist dose needed to produce antinociception in an inflammatory pain model. Pain. 2015;156:849-58 pubmed publisher
Silva G, Lopes P, Fonoff E, Pagano R. The spinal anti-inflammatory mechanism of motor cortex stimulation: cause of success and refractoriness in neuropathic pain?. J Neuroinflammation. 2015;12:10 pubmed publisher
Lee K, Royston S, Vest M, Ley D, Lee S, Bolton E, et al. N-methyl-D-aspartate receptors mediate activity-dependent down-regulation of potassium channel genes during the expression of homeostatic intrinsic plasticity. Mol Brain. 2015;8:4 pubmed publisher
Mesirca P, Alig J, Torrente A, MÃ¼ller J, Marger L, Rollin A, et al. Cardiac arrhythmia induced by genetic silencing of 'funny' (f) channels is rescued by GIRK4 inactivation. Nat Commun. 2014;5:4664 pubmed publisher
Morandini A, Ramos Junior E, Potempa J, Nguyen K, Oliveira A, Bellio M, et al. Porphyromonas gingivalis fimbriae dampen P2X7-dependent interleukin-1β secretion. J Innate Immun. 2014;6:831-45 pubmed publisher
Ambrosini E, Sicca F, Brignone M, D Adamo M, Napolitano C, Servettini I, et al. Genetically induced dysfunctions of Kir2.1 channels: implications for short QT3 syndrome and autism-epilepsy phenotype. Hum Mol Genet. 2014;23:4875-86 pubmed publisher
Belkouch M, Dansereau M, Tétreault P, Biet M, Beaudet N, Dumaine R, et al. Functional up-regulation of Nav1.8 sodium channel in A? afferent fibers subjected to chronic peripheral inflammation. J Neuroinflammation. 2014;11:45 pubmed publisher
Sorrell M, Hauser K. Ligand-gated purinergic receptors regulate HIV-1 Tat and morphine related neurotoxicity in primary mouse striatal neuron-glia co-cultures. J Neuroimmune Pharmacol. 2014;9:233-44 pubmed publisher
Cao Z, Yu Y, Wu Y, Hao P, Di Z, He Y, et al. The genome of Mesobuthus martensii reveals a unique adaptation model of arthropods. Nat Commun. 2013;4:2602 pubmed publisher
Hammelmann V, Zong X, Hofmann F, Michalakis S, Biel M. The cGMP-dependent protein kinase II Is an inhibitory modulator of the hyperpolarization-activated HCN2 channel. PLoS ONE. 2011;6:e17078 pubmed publisher
Gazula V, Strumbos J, Mei X, Chen H, Rahner C, Kaczmarek L. Localization of Kv1.3 channels in presynaptic terminals of brainstem auditory neurons. J Comp Neurol. 2010;518:3205-20 pubmed publisher
Amadio S, Montilli C, Picconi B, Calabresi P, Volonte C. Mapping P2X and P2Y receptor proteins in striatum and substantia nigra: An immunohistological study. Purinergic Signal. 2007;3:389-98 pubmed publisher
Amadio S, Vacca F, Martorana A, Sancesario G, Volonte C. P2Y1 receptor switches to neurons from glia in juvenile versus neonatal rat cerebellar cortex. BMC Dev Biol. 2007;7:77 pubmed
Storey N, Latchman D, Bevan S. Selective internalization of sodium channels in rat dorsal root ganglion neurons infected with herpes simplex virus-1. J Cell Biol. 2002;158:1251-62 pubmed
Mori Y, Wakamori M, Miyakawa T, Hermosura M, Hara Y, Nishida M, et al. Transient receptor potential 1 regulates capacitative Ca(2+) entry and Ca(2+) release from endoplasmic reticulum in B lymphocytes. J Exp Med. 2002;195:673-81 pubmed

image

image 1 :

Alomone Labs XE991 blocks KCNQ2/KCNQ3 channels heterologously expressed inXenopusoocytes. - 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 MXE991(#X-100) inhibits the KCNQ2/KCNQ3 current in a reversible manner (indicated by the horizontal bar). B. Representative current traces before and during application of 100 M XE991 as indicated.

product information

CAT :

X-100

SKU :

X-100_10 mg

Product Name :

XE991

Group Type :

Non Antibodies

Product Type :

S. Molecules

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

Product Page - Scientific background :

Voltage-gated K+ channels of the KCNQ family (KV7) 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 KV7.2 + KV7.3 (KCNQ2 + KCNQ3)/M-currents (IC50 = 0.6 μM) and KV7.1 (KCNQ1) homomeric channels (IC50 = 0.75 μM) but is less potent against KV7.1/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.

Supplier :

Alomone Labs

Target :

KCNQ K+ channels

Long Description :

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

Short Description :

A Blocker of KCNQ Channels

MW :

376.45

Source :

Synthetic

Molecular formula :

C26H20N2O.

Effective Concentration :

0.1-300 µM.

Reconstitution and Solubility :

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

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.

Lead Time :

1-2 Business Days

Country of origin :

Israel/IL

Applications key :

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

Purity :

>95%

CAS No :

122955-42-4

Form :

Lyophilized powder.

Comment :

Contact Alomone Labs for technical support and product customization

UNSPSC :

41116134

Bioassay Tested :

Yes

Cited Application :

Electrophysiology

Chemical Name :

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

more info or order :

Alomone Labs product webpage