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A 438079 hydrochloride

Catalog #: 2972
45 Citations Datasheet
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A 438079 hydrochloride | CAS No. 899431-18-6 | P2X Receptor Antagonists
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Description: Competitive P2X7 antagonist

Chemical Name: 3-[[5-(2,3-Dichlorophenyl)-1H-tetrazol-1-yl]methyl]pyridine hydrochloride

Purity: ≥98%

Product Details
Citations (45)
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Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

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 μM). Possesses antinociceptive activity in models of neuropathic pain in vivo. Inhibits methamphetamine-induced microglial migration and phagocytosis in vitro.

Technical Data

M.Wt:
342.61
Formula:
C13H9Cl2N5.HCl
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Desiccate at RT
CAS No:
899431-18-6

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.

Background References

  1. Slc11a1 (Nramp1) impairs growth of Salmonella enterica serovar typhimurium in macrophages via stimulation of lipocalin-2 expression.
    Fritsche G, Nairz M, Libby S, Fang F, Weiss G
    J Leukoc Biol, 2012;92(2):353-9.
  2. Overexpression of CD39 in mouse airways promotes bacteria-induced inflammation.

    J. Immunol., 2012;189(4):1966-74.
  3. The ATP Receptors P2X7 and P2X4 Modulate High Glucose and Palmitate-Induced Inflammatory Responses in Endothelial Cells.
    Sathanoori R, Sward K, Olde B, Erlinge D
    PLoS ONE, 2015;10(5):e0125111.
  4. P2RX7 sensitizes Mac-1/ICAM-1-dependent leukocyte-endothelial adhesion and promotes neurovascular injury during septic encephalopathy.
    Wang H, Hong L, Huang J, Jiang Q, Tao R, Tan C, Lu N, Wang C, Ahmed M, Lu Y, Liu Z, Shi W, Lai E, Wilcox C, Han F
    Cell Res, 2015;25(6):674-90.
  5. Purinergic P2X7 receptor drives T cell lineage choice and shapes peripheral gamma/delta cells.
    Frascoli M, Marcandalli J, Schenk U, Grassi F
    J. Immunol., 2012;189(1):174-80.
  6. Activation of neuronal P2X7 receptor-pannexin-1 mediates death of enteric neurons during colitis.
    Gulbransen BD, Bashashati M, Hirota SA
    Nat. Med., 2012;18(4):600-4.
  7. A negative feedback loop mediated by STAT3 limits human Th17 responses.
    Purvis H, Anderson A, Young D, Isaacs J, Hilkens C
    J Immunol, 2015;193(3):1142-50.
  8. Type I IFNs and IL-18 regulate the antiviral response of primary human gammadelta T cells against dendritic cells infected with Dengue virus.
    Tsai C, Liong K, Gunalan M, Li N, Lim D, Fisher D, Macary P, Leo Y, Wong S, Puan K, Wong S
    J Immunol, 2015;194(8):3890-900.
  9. Interleukin-18 activates Vg9Vd2+ T cells from HIV+ Individuals: Recovering the Response to Phosphoantigen
    AS Murday, S Chaudhry, CD Pauza
    Immunology, 2017;0(0):.
  10. P2X7 receptor antagonism prevents IL-1? release from salivary epithelial cells and reduces inflammation in a mouse model of autoimmune exocrinopathy
    MG Khalafalla, LT Woods, JM Camden, AA Khan, KH Limesand, MJ Petris, L Erb, GA Weisman
    J. Biol. Chem., 2017;0(0):.
  11. A central role for P2X7 receptors in human microglia
    L Janks, CVR Sharma, TM Egan
    J Neuroinflammation, 2018;15(1):325.
  12. Brain micro-inflammation at specific vessels dysregulates organ-homeostasis via the activation of a new neural circuit
    Y Arima, T Ohki, N Nishikawa, K Higuchi, M Ota, Y Tanaka, J Nio-Kobaya, M Elfeky, R Sakai, Y Mori, T Kawamoto, A Stofkova, Y Sakashita, Y Morimoto, M Kuwatani, T Iwanaga, Y Yoshioka, N Sakamoto, A Yoshimura, M Takiguchi, S Sakoda, M Prinz, D Kamimura, M Murakami
    Elife, 2017;6(0):.
  13. Ezrin/radixin/moesin are required for the purinergic P2X7 receptor (P2X7R)-dependent processing of the amyloid precursor protein.
    Darmellah A, Rayah A, Auger R, Cuif M, Prigent M, Arpin M, Alcover A, Delarasse C, Kanellopoulos J
    J Biol Chem, 2012;287(41):34583-95.
  14. Involvement of the chemokine CCL3 and the purinoceptor P2X7 in the spinal cord in paclitaxel-induced mechanical allodynia.
    Ochi-ishi, Ryutaro, Nagata, Kenichir, Inoue, Tomoyuki, Tozaki-Saitoh, Hidetosh, Tsuda, Makoto, Inoue, Kazuhide
    Mol Pain, 2014;10(0):53.
  15. Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
    Nelson et al.
    J.Med.Chem., 2006;49:3659
  16. Discovery of P2X7 receptor-selective antagonists offers new insights into P2X7 receptor function and indicates a role in chronic pain states.
    Donnelly-Roberts and Jarvis
    Br.J.Pharmacol., 2007;151:571
  17. P2X7-related modulation of pathological nociception in rats.
    McGaraughty et al.
    Neuroscience, 2007;146:1817
  18. Methamphetamine alters microglial immune function through P2X7R signaling.
    Fernandes et al.
    J.Neuroinflammation., 2016;13:91
  19. Serum Amyloid A1 is an epithelial pro-restitutive factor
    BH Hinrichs, JD Matthews, D Siuda, MN O'Leary, AA Wolfarth, BJ Saeedi, A Nusrat, AS Neish
    Am. J. Pathol., 2018;0(0):.

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Citations for A 438079 hydrochloride

The citations listed below are publications that use Tocris products. Selected citations for A 438079 hydrochloride include:

45 Citations: Showing 1 - 10

  1. Extracellular ATP Increases Glucose Metabolism in Skeletal Muscle Cells in a P2 Receptor Dependent Manner but Does Not Contribute to Palmitate-Induced Insulin Resistance.
    Authors: Miguel Cruz & Beall
    Front Physiol  2020;11
  2. Amyloid Peptide Induced Neuroinflammation Increases the P2X7 Receptor Expression in Microglial Cells, Impacting on Its Functionality.
    Authors: Martínez-Frailes Et al.
    Front Cell Neurosci  2019;13:143
  3. ATP-mediated Events in Peritubular Cells Contribute to Sterile Testicular Inflammation.
    Authors: Walenta Et al.
    Sci Rep  2018;8:1431
  4. Activator protein-1 contributes to the NaCl-induced expression of VEGF and PlGF in RPE cells.
    Authors: Kleiner Et al.
    Mol Vis  2018;24:647
  5. Targeting the NLRP3 inflammasome to attenuate spinal cord injury in mice.
    Authors: Jiang
    J Neuroinflammation  2017;14(1):207
  6. Neutrophil P2X7 receptors mediate NLRP3 inflammasome-dependent IL-1β secretion in response to ATP.
    Authors: Karmakar Et al.
    Nat.Commun.  2016;7:10555
  7. Mitochondrial Dysfunction, Depleted Purinergic Signaling, and Defective T Cell Vigilance and Immune Defense.
    Authors: Ledderose Et al.
    J Infect Dis  2016;213:456
  8. Active Caspase-1 Induces Plasma Membrane Pores That Precede Pyroptotic Lysis and Are Blocked by Lanthanides
    Authors: Russo Et al.
    The Journal of Immunology  2016;197:1353
  9. Neuronal Release of Cytokine IL-3 Triggered by Mechanosensitive Autostimulation of the P2X7 Receptor Is Neuroprotective.
    Authors: Lim Et al.
    Front Cell Neurosci  2016;10:270
  10. Modulation of P2X4/P2X7/Pannexin-1 sensitivity to extracellular ATP via iverm. induces a non-apoptotic and inflammatory form of cancer cell death.
    Authors: Draganov Et al.
    Autophagy  2015;5:16222
  11. P2RX7 sensitizes Mac-1/ICAM-1-dependent leukocyte-endothelial adhesion and promotes neurovascular injury during septic encephalopathy.
    Authors: Wang Et al.
    Cell Res  2015;25:674
  12. Nucleotide receptors control IL-8/CXCL8 and MCP-1/CCL2 secretions as well as proliferation in human glioma cells.
    Authors: Braganhol Et al.
    Biochim Biophys Acta  2015;1852:120
  13. Selected ginsenosides of the protopanaxdiol series are novel positive allosteric modulators of P2X7 receptors.
    Authors: Helliwell Et al.
    Br J Pharmacol  2015;172:3326
  14. The P2X7 receptor regulates cell survival, migration and invasion of pancreatic ductal adenocarcinoma cells.
    Authors: Giannuzzo Et al.
    J Neurosci  2015;14:203
  15. Bile acid effects are mediated by ATP release and purinergic signalling in exocrine pancreatic cells.
    Authors: Kowal Et al.
    Mol Cancer  2015;13:28
  16. A novel mechanism of autophagic cell death in dystrophic muscle regulated by P2RX7 receptor large-pore formation and HSP90.
    Authors: Young Et al.
    J Cell Sci  2015;11:113
  17. The ATP Receptors P2X7 and P2X4 Modulate High Glucose and Palmitate-Induced Inflammatory Responses in Endothelial Cells.
    Authors: Sathanoori Et al.
    PLoS One  2015;10:e0125111
  18. Extracellular ATP does not induce P2X7 receptor-dependent responses in cultured renal- and liver-derived swine macrophages.
    Authors: Takenouchi Et al.
    Purinergic Signal  2014;4:62
  19. Tanshinone II A sulfonate, but not tanshinone II A, acts as potent negative allosteric modulator of the human purinergic receptor P2X7.
    Authors: Kaiser Et al.
    J Pharmacol Exp Ther  2014;350:531
  20. Involvement of the chemokine CCL3 and the purinoceptor P2X7 in the spinal cord in PacT.-induced mechanical allodynia.
    Authors: Ochi-Ishi Et al.
    Biochem Biophys Res Commun  2014;10:53
  21. Enhanced autophagy blocks angiogenesis via degradation of gastrin-releasing peptide in neuroblastoma cells.
    Authors: Kim Et al.
    Cell Commun Signal  2013;9:1579
  22. Pharmacological characterization of the P2 receptors profile in the podocytes of the freshly isolated rat glomeruli.
    Authors: Ilatovskaya Et al.
    Am J Physiol Cell Physiol  2013;305:C1050
  23. Mitochondrial superoxide generation enhances P2X7R-mediated loss of cell surface CD62L on naive human CD4+ T lymphocytes.
    Authors: Foster Et al.
    J Immunol  2013;190:1551
  24. Natural compounds with P2X7 receptor-modulating properties.
    Authors: Fischer Et al.
    Purinergic Signal  2013;10:313
  25. ATP release and autocrine signaling through P2X4 receptors regulate γδ T cell activation.
    Authors: Manohar Et al.
    J Leukoc Biol  2012;92:787
  26. P2X7 receptor activation mediates organic cation uptake into human myeloid leukaemic KG-1 cells.
    Authors: Gadeock Et al.
    Neurosci Lett  2012;8:669
  27. Involvement of connexin43 hemichannel in ATP release after γ-irradiation.
    Authors: Ohshima Et al.
    Mol Pain  2012;53:551
  28. Regulation of P2X7-dependent inflammatory functions by P2X4 receptor in mouse macrophages.
    Authors: Kawano Et al.
    Results Immunol  2012;420:102
  29. P2X7 receptor-mediated purinergic signaling promotes liver injury in acetaminophen hepatotoxicity in mice.
    Authors: Hoque Et al.
    Am J Physiol Gastrointest Liver Physiol  2012;302:G1171
  30. P2X?-mediated calcium influx triggers a sustained, PI3K-dependent increase in metabolic acid production by osteoblast-like cells.
    Authors: Grol Et al.
    Am J Physiol Endocrinol Metab  2012;302:E561
  31. Mechanisms of ATP release by human trabecular meshwork cells, the enabling step in purinergic regulation of aqueous humor outflow.
    Authors: Li Et al.
    J Cell Physiol  2012;227:172
  32. ATP induces protein arginine deiminase 2-dependent citrullination in mast cells through the P2X7 purinergic receptor.
    Authors: Arandjelovic Et al.
    J Immunol  2012;189:4112
  33. Positive allosteric modulation by iverm. of human but not murine P2X7 receptors.
    Authors: Nörenberg Et al.
    Br J Pharmacol  2012;167:48
  34. P2X7 receptor activation ameliorates CA3 neuronal damage via a tumor necrosis factor-α-mediated pathway in the rat hippocampus following status epilepticus.
    Authors: Kim Et al.
    J Neuroinflammation  2011;8:62
  35. Purinergic signaling induces cyclooxygenase-1-dependent prostanoid synthesis in microglia: roles in the outcome of excitotoxic brain injury.
    Authors: Anrather Et al.
    PLoS One  2011;6:e25916
  36. The P2X7-Egr pathway regulates nucleotide-dependent inflammatory gene expression in microglia.
    Authors: Friedle Et al.
    Glia  2011;59:1
  37. Clemastine potentiates the human P2X7 receptor by sensitizing it to lower ATP concentrations.
    Authors: Nörenberg Et al.
    J Biol Chem  2011;286:11067
  38. Tissue-nonspecific alkaline phosphatase promotes axonal growth of hippocampal neurons.
    Authors: Díez-Zaera Et al.
    Mol Biol Cell  2011;22:1014
  39. P2X(7) receptor antagonists display agonist-like effects on cell signaling proteins.
    Authors: Hedden Et al.
    Biochim Biophys Acta  2011;1810:532
  40. The P2X7 receptor-pannexin-1 complex decreases muscarinic acetylcholine receptor-mediated seizure susceptibility in mice.
    Authors: Kim
    J Clin Invest  2011;121:2037
  41. Hypertonic stress regulates T cell function via pannexin-1 hemichannels and P2X receptors.
    Authors: Woehrle Et al.
    J Leukoc Biol  2010;88:1181
  42. P2X7-dependent release of interleukin-1β and nociception in the spinal cord following lipopolysaccharide.
    Authors: Clark Et al.
    J Radiat Res  2010;30:573
  43. Temporal interleukin-1beta secretion from primary human peripheral blood monocytes by P2X7-independent and P2X7-dependent mechanisms.
    Authors: Ward Et al.
    J Biol Chem  2010;285:23147
  44. Involvement of SLC17A9-dependent vesicular exocytosis in the mechanism of ATP release during T cell activation.
    Authors: Tokunaga Et al.
    J Biol Chem  2010;285:17406
  45. Inhibition of the ATP-gated P2X7 receptor promotes axonal growth and branching in cultured hippocampal neurons.
    Authors: Díaz-Hernández Et al.
    Autophagy  2008;121:3717

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