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company name :
Tocris Bioscience
product type :
chemical
product name :
A 438079 hydrochloride
catalog :
2972/10
quantity :
10 mg (also 50 mg)
price :
251 USD
more info or order :
citations: 57
Reference
Cruz A, Beall C. Extracellular ATP Increases Glucose Metabolism in Skeletal Muscle Cells in a P2 Receptor Dependent Manner but Does Not Contribute to Palmitate-Induced Insulin Resistance. Front Physiol. 2020;11:567378 pubmed publisher
Martínez Frailes C, di Lauro C, Bianchi C, de Diego García L, Sebastián Serrano A, Bosca L, et al. Amyloid Peptide Induced Neuroinflammation Increases the P2X7 Receptor Expression in Microglial Cells, Impacting on Its Functionality. Front Cell Neurosci. 2019;13:143 pubmed publisher
Janks L, Sharma C, Egan T. A central role for P2X7 receptors in human microglia. J Neuroinflammation. 2018;15:325 pubmed publisher
Kleiner J, Hollborn M, Wiedemann P, Bringmann A. Activator protein-1 contributes to the NaCl-induced expression of VEGF and PlGF in RPE cells. Mol Vis. 2018;24:647-666 pubmed
Hinrichs B, Matthews J, Siuda D, O Leary M, Wolfarth A, Saeedi B, et al. Serum Amyloid A1 Is an Epithelial Prorestitutive Factor. Am J Pathol. 2018;188:937-949 pubmed publisher
Walenta L, FLECK D, Frohlich T, von Eysmondt H, Arnold G, Spehr J, et al. ATP-mediated Events in Peritubular Cells Contribute to Sterile Testicular Inflammation. Sci Rep. 2018;8:1431 pubmed publisher
Jiang W, Li M, He F, Zhou S, Zhu L. Targeting the NLRP3 inflammasome to attenuate spinal cord injury in mice. J Neuroinflammation. 2017;14:207 pubmed publisher
Arima Y, Ohki T, Nishikawa N, Higuchi K, Ota M, Tanaka Y, et al. Brain micro-inflammation at specific vessels dysregulates organ-homeostasis via the activation of a new neural circuit. elife. 2017;6: pubmed publisher
Khalafalla M, Woods L, Camden J, Khan A, Limesand K, Petris M, et al. P2X7 receptor antagonism prevents IL-1? release from salivary epithelial cells and reduces inflammation in a mouse model of autoimmune exocrinopathy. J Biol Chem. 2017;292:16626-16637 pubmed publisher
Murday A, Chaudhry S, Pauza C. Interleukin-18 activates V?9V?2+ T cells from HIV-positive individuals: recovering the response to phosphoantigen. Immunology. 2017;151:385-394 pubmed publisher
Lim J, Lu W, Beckel J, Mitchell C. Neuronal Release of Cytokine IL-3 Triggered by Mechanosensitive Autostimulation of the P2X7 Receptor Is Neuroprotective. Front Cell Neurosci. 2016;10:270 pubmed
Liu J, Talebian F, Wu L, Liu Z, Li M, Wu L, et al. A Critical Role for CD200R Signaling in Limiting the Growth and Metastasis of CD200+ Melanoma. J Immunol. 2016;197:1489-97 pubmed publisher
Karmakar M, Katsnelson M, Dubyak G, Pearlman E. Neutrophil P2X7 receptors mediate NLRP3 inflammasome-dependent IL-1β secretion in response to ATP. Nat Commun. 2016;7:10555 pubmed publisher
Giannuzzo A, Pedersen S, Novak I. The P2X7 receptor regulates cell survival, migration and invasion of pancreatic ductal adenocarcinoma cells. Mol Cancer. 2015;14:203 pubmed publisher
Draganov D, Gopalakrishna Pillai S, Chen Y, Zuckerman N, Moeller S, Wang C, et al. Modulation of P2X4/P2X7/Pannexin-1 sensitivity to extracellular ATP via Ivermectin induces a non-apoptotic and inflammatory form of cancer cell death. Sci Rep. 2015;5:16222 pubmed publisher
Ledderose C, Bao Y, Ledderose S, Woehrle T, Heinisch M, Yip L, et al. Mitochondrial Dysfunction, Depleted Purinergic Signaling, and Defective T Cell Vigilance and Immune Defense. J Infect Dis. 2016;213:456-64 pubmed publisher
Kowal J, Haanes K, Christensen N, Novak I. Bile acid effects are mediated by ATP release and purinergic signalling in exocrine pancreatic cells. Cell Commun Signal. 2015;13:28 pubmed publisher
Wang H, Hong L, Huang J, Jiang Q, Tao R, Tan C, et al. P2RX7 sensitizes Mac-1/ICAM-1-dependent leukocyte-endothelial adhesion and promotes neurovascular injury during septic encephalopathy. Cell Res. 2015;25:674-90 pubmed publisher
Sathanoori R, Swärd K, Olde B, Erlinge D. The ATP Receptors P2X7 and P2X4 Modulate High Glucose and Palmitate-Induced Inflammatory Responses in Endothelial Cells. PLoS ONE. 2015;10:e0125111 pubmed publisher
Helliwell R, ShioukHuey C, Dhuna K, Molero J, Ye J, Xue C, et al. Selected ginsenosides of the protopanaxdiol series are novel positive allosteric modulators of P2X7 receptors. Br J Pharmacol. 2015;172:3326-40 pubmed publisher
Tsai C, Liong K, Gunalan M, Li N, Lim D, Fisher D, et al. Type I IFNs and IL-18 regulate the antiviral response of primary human γδ T cells against dendritic cells infected with Dengue virus. J Immunol. 2015;194:3890-900 pubmed publisher
Young C, Sinadinos A, Lefebvre A, Chan P, Arkle S, Vaudry D, et al. A novel mechanism of autophagic cell death in dystrophic muscle regulated by P2RX7 receptor large-pore formation and HSP90. Autophagy. 2015;11:113-30 pubmed publisher
Braganhol E, Kukulski F, Lévesque S, Fausther M, Lavoie E, Zanotto Filho A, et al. Nucleotide receptors control IL-8/CXCL8 and MCP-1/CCL2 secretions as well as proliferation in human glioma cells. Biochim Biophys Acta. 2015;1852:120-30 pubmed publisher
Takenouchi T, Suzuki S, Shinkai H, Tsukimoto M, Sato M, Uenishi H, et al. Extracellular ATP does not induce P2X7 receptor-dependent responses in cultured renal- and liver-derived swine macrophages. Results Immunol. 2014;4:62-7 pubmed publisher
Ochi ishi R, Nagata K, Inoue T, Tozaki Saitoh H, Tsuda M, Inoue K. Involvement of the chemokine CCL3 and the purinoceptor P2X7 in the spinal cord in paclitaxel-induced mechanical allodynia. Mol Pain. 2014;10:53 pubmed publisher
Purvis H, Anderson A, Young D, Isaacs J, Hilkens C. A negative feedback loop mediated by STAT3 limits human Th17 responses. J Immunol. 2014;193:1142-50 pubmed publisher
Kaiser M, Sobottka H, Fischer W, Schaefer M, Nörenberg W. Tanshinone II A sulfonate, but not tanshinone II A, acts as potent negative allosteric modulator of the human purinergic receptor P2X7. J Pharmacol Exp Ther. 2014;350:531-42 pubmed publisher
Fischer W, Urban N, Immig K, Franke H, Schaefer M. Natural compounds with P2X7 receptor-modulating properties. Purinergic Signal. 2014;10:313-26 pubmed publisher
Kim K, Paul P, Qiao J, Lee S, Chung D. Enhanced autophagy blocks angiogenesis via degradation of gastrin-releasing peptide in neuroblastoma cells. Autophagy. 2013;9:1579-90 pubmed publisher
Ilatovskaya D, Palygin O, Levchenko V, Staruschenko A. Pharmacological characterization of the P2 receptors profile in the podocytes of the freshly isolated rat glomeruli. Am J Physiol Cell Physiol. 2013;305:C1050-9 pubmed publisher
Foster J, Carter E, Kilty I, Mackenzie A, Ward S. Mitochondrial superoxide generation enhances P2X7R-mediated loss of cell surface CD62L on naive human CD4+ T lymphocytes. J Immunol. 2013;190:1551-9 pubmed publisher
Arandjelovic S, McKenney K, Leming S, Mowen K. ATP induces protein arginine deiminase 2-dependent citrullination in mast cells through the P2X7 purinergic receptor. J Immunol. 2012;189:4112-22 pubmed publisher
Darmellah A, Rayah A, Auger R, Cuif M, Prigent M, Arpin M, et al. Ezrin/radixin/moesin are required for the purinergic P2X7 receptor (P2X7R)-dependent processing of the amyloid precursor protein. J Biol Chem. 2012;287:34583-95 pubmed publisher
Ohshima Y, Tsukimoto M, Harada H, Kojima S. Involvement of connexin43 hemichannel in ATP release after ?-irradiation. J Radiat Res. 2012;53:551-7 pubmed publisher
Th xe9 xe2 tre E, Frederix K, Guilmain W, Delierneux C, Lecut C, Bettendorff L, et al. Overexpression of CD39 in mouse airways promotes bacteria-induced inflammation. J Immunol. 2012;189:1966-74 pubmed publisher
Manohar M, Hirsh M, Chen Y, Woehrle T, Karande A, Junger W. ATP release and autocrine signaling through P2X4 receptors regulate ?? T cell activation. J Leukoc Biol. 2012;92:787-94 pubmed publisher
Fritsche G, Nairz M, Libby S, Fang F, Weiss G. Slc11a1 (Nramp1) impairs growth of Salmonella enterica serovar typhimurium in macrophages via stimulation of lipocalin-2 expression. J Leukoc Biol. 2012;92:353-9 pubmed publisher
Gadeock S, Pupovac A, Sluyter V, Spildrejorde M, Sluyter R. P2X7 receptor activation mediates organic cation uptake into human myeloid leukaemic KG-1 cells. Purinergic Signal. 2012;8:669-76 pubmed publisher
Frascoli M, Marcandalli J, Schenk U, Grassi F. Purinergic P2X7 receptor drives T cell lineage choice and shapes peripheral ?? cells. J Immunol. 2012;189:174-80 pubmed publisher
Nörenberg W, Sobottka H, Hempel C, Plötz T, Fischer W, Schmalzing G, et al. Positive allosteric modulation by ivermectin of human but not murine P2X7 receptors. Br J Pharmacol. 2012;167:48-66 pubmed publisher
Gulbransen B, Bashashati M, Hirota S, Gui X, Roberts J, MacDonald J, et al. Activation of neuronal P2X7 receptor-pannexin-1 mediates death of enteric neurons during colitis. Nat Med. 2012;18:600-4 pubmed publisher
Kawano A, Tsukimoto M, Mori D, Noguchi T, Harada H, Takenouchi T, et al. Regulation of P2X7-dependent inflammatory functions by P2X4 receptor in mouse macrophages. Biochem Biophys Res Commun. 2012;420:102-7 pubmed publisher
Hoque R, Sohail M, Salhanick S, Malik A, Ghani A, Robson S, et al. P2X7 receptor-mediated purinergic signaling promotes liver injury in acetaminophen hepatotoxicity in mice. Am J Physiol Gastrointest Liver Physiol. 2012;302:G1171-9 pubmed publisher
Grol M, Zelner I, Dixon S. P2X?-mediated calcium influx triggers a sustained, PI3K-dependent increase in metabolic acid production by osteoblast-like cells. Am J Physiol Endocrinol Metab. 2012;302:E561-75 pubmed publisher
Anrather J, Gallo E, Kawano T, Orio M, Abe T, Gooden C, et al. Purinergic signaling induces cyclooxygenase-1-dependent prostanoid synthesis in microglia: roles in the outcome of excitotoxic brain injury. PLoS ONE. 2011;6:e25916 pubmed publisher
Kim J, Ryu H, Kang T. P2X7 receptor activation ameliorates CA3 neuronal damage via a tumor necrosis factor-?-mediated pathway in the rat hippocampus following status epilepticus. J Neuroinflammation. 2011;8:62 pubmed publisher
Kim J, Kang T. The P2X7 receptor-pannexin-1 complex decreases muscarinic acetylcholine receptor-mediated seizure susceptibility in mice. J Clin Invest. 2011;121:2037-47 pubmed publisher
Hedden L, Benes C, Soltoff S. P2X(7) receptor antagonists display agonist-like effects on cell signaling proteins. Biochim Biophys Acta. 2011;1810:532-42 pubmed publisher
Li A, Leung C, Peterson Yantorno K, Stamer W, Mitchell C, Civan M. Mechanisms of ATP release by human trabecular meshwork cells, the enabling step in purinergic regulation of aqueous humor outflow. J Cell Physiol. 2012;227:172-82 pubmed publisher
Diez Zaera M, Diaz Hernandez J, Hernández Álvarez E, Zimmermann H, Diaz Hernandez M, Miras Portugal M. Tissue-nonspecific alkaline phosphatase promotes axonal growth of hippocampal neurons. Mol Biol Cell. 2011;22:1014-24 pubmed publisher
Nörenberg W, Hempel C, Urban N, Sobottka H, Illes P, Schaefer M. Clemastine potentiates the human P2X7 receptor by sensitizing it to lower ATP concentrations. J Biol Chem. 2011;286:11067-81 pubmed publisher
Woehrle T, Yip L, Manohar M, Sumi Y, Yao Y, Chen Y, et al. Hypertonic stress regulates T cell function via pannexin-1 hemichannels and P2X receptors. J Leukoc Biol. 2010;88:1181-9 pubmed publisher
Friedle S, Brautigam V, Nikodemova M, Wright M, Watters J. The P2X7-Egr pathway regulates nucleotide-dependent inflammatory gene expression in microglia. Glia. 2011;59:1-13 pubmed publisher
Ward J, West P, Ariaans M, Parker L, Francis S, Crossman D, et al. Temporal interleukin-1beta secretion from primary human peripheral blood monocytes by P2X7-independent and P2X7-dependent mechanisms. J Biol Chem. 2010;285:23147-58 pubmed publisher
Tokunaga A, Tsukimoto M, Harada H, Moriyama Y, Kojima S. Involvement of SLC17A9-dependent vesicular exocytosis in the mechanism of ATP release during T cell activation. J Biol Chem. 2010;285:17406-16 pubmed publisher
Clark A, Staniland A, Marchand F, Kaan T, McMahon S, Malcangio M. P2X7-dependent release of interleukin-1beta and nociception in the spinal cord following lipopolysaccharide. J Neurosci. 2010;30:573-82 pubmed publisher
Diaz Hernandez M, del Puerto A, Díaz Hernández J, Diez Zaera M, Lucas J, Garrido J, et al. Inhibition of the ATP-gated P2X7 receptor promotes axonal growth and branching in cultured hippocampal neurons. J Cell Sci. 2008;121:3717-28 pubmed publisher
product information
brand :
Tocris, a Bio-Techne brand
catalog number base :
2972
SKU :
2972/10
product name :
A 438079 hydrochloride
description :
Competitive P2X7 antagonist
target :
P2X Receptor Antagonists
unit size :
10 mg (also 50 mg)
category :
Small Molecules
purity :
98%
storage :
Desiccate at RT
observed molecular weight :
342.61
url print :
?utm_source=biocompare&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
A 438079 hydrochloride is a competitive P2X7 receptor antagonist (pIC50 = 6.9 for the inhibition of Ca2+ influx in the human recombinant P2X7 cell line). Devoid of activity at other P2 receptors (IC50 10 u M). Possesses antinociceptive activity in models of neuropathic pain in vivo . Inhibits methamphetamine-induced microglial migration and phagocytosis in vitro .
product keywords :
Competitve P2X7 antagonists Receptors Purinergic purinoceptors A438079 hydrochloride P2X Receptors 2972,
extended description :
Competitive P2X7 antagonist
chemical name text :
3-[[5-(2,3-Dichlorophenyl)-1H-tetrazol-1-yl]methyl]pyridine hydrochloride
formula :
C13H9Cl2N5.HCl
formula text :
C13H9Cl2N5.HCl
cas num :
899431-18-6
USD :
240
USD 2025 :
251 USD
product details :
Competitive P2X7 antagonist
more info or order :
company information
Tocris Bioscience
The Watkins Building
Atlantic Road
Avonmouth, Bristol
BS11 9QD
info@bio-techne.com
https://www.tocris.com
800-343-7475
headquarters: UK