A 438079 hydrochloride

Name: A 438079 hydrochloride
Brand: Tocris Bioscience
SKU: 2972

Tocris Bioscience, part of Bio-Techne | Catalog # 2972

Citations (47)

COA / SDS

Competitive P2X7 antagonist

Key Product Details

Chemical Name:	3-[[5-(2,3-Dichlorophenyl)-1H-tetrazol-1-yl]methyl]pyridine hydrochloride
Purity:	≥98%
Molecular Weight:	342.61 kDa

View Full Technical Details for A 438079 hydrochloride

Technical Data
Citations

Biological Activity for A 438079 hydrochloride

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 for A 438079 hydrochloride

M. Wt	342.61 kDa
Formula	C₁₃H₉Cl₂N₅.HCl
Storage	Desiccate at RT
Purity	≥98%
CAS Number	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.

Solubility for A 438079 hydrochloride

Solubility

Soluble Soluble to 100 mM in DMSO

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References for A 438079 hydrochloride

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

Darmellah A, Rayah A, Auger R, Cuif M, Prigent M, Arpin M, Alcover A, Delarasse C, Kanellopoulos J Ezrin/radixin/moesin are required for the purinergic P2X7 receptor (P2X7R)-dependent processing of the amyloid precursor protein. J Biol Chem, 2012;287(41):34583-95. 2012 PMID: 22891241
Sathanoori R, Sward 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(5):e0125111. 2015 PMID: 25938443
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 Brain micro-inflammation at specific vessels dysregulates organ-homeostasis via the activation of a new neural circuit Elife, 2017;6(0):. 2017 PMID: 28809157
AS Murday, S Chaudhry, CD Pauza Interleukin-18 activates Vg9Vd2+ T cells from HIV+ Individuals: Recovering the Response to Phosphoantigen Immunology, 2017;0(0):. 2017 PMID: 28342224
MG Khalafalla, LT Woods, JM Camden, AA Khan, KH Limesand, MJ Petris, L Erb, GA Weisman 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;0(0):. 2017 PMID: 28798231
Purvis H, Anderson A, Young D, Isaacs J, Hilkens C A negative feedback loop mediated by STAT3 limits human Th17 responses. J Immunol, 2015;193(3):1142-50. 2015 PMID: 24973454
Tsai C, Liong K, Gunalan M, Li N, Lim D, Fisher D, Macary P, Leo Y, Wong S, Puan K, Wong S Type I IFNs and IL-18 regulate the antiviral response of primary human gammadelta T cells against dendritic cells infected with Dengue virus. J Immunol, 2015;194(8):3890-900. 2015 PMID: 25732728
Gulbransen BD, Bashashati M, Hirota SA Activation of neuronal P2X7 receptor-pannexin-1 mediates death of enteric neurons during colitis. Nat. Med., 2012;18(4):600-4. 2012 PMID: 22426419
Frascoli M, Marcandalli J, Schenk U, Grassi F Purinergic P2X7 receptor drives T cell lineage choice and shapes peripheral gamma/delta cells. J. Immunol., 2012;189(1):174-80. 2012 PMID: 22649196
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 P2RX7 sensitizes Mac-1/ICAM-1-dependent leukocyte-endothelial adhesion and promotes neurovascular injury during septic encephalopathy. Cell Res, 2015;25(6):674-90. 2015 PMID: 25998681
Ochi-ishi, Ryutaro, Nagata, Kenichir, Inoue, Tomoyuki, Tozaki-Saitoh, Hidetosh, Tsuda, Makoto, Inoue, Kazuhide Involvement of the chemokine CCL3 and the purinoceptor P2X7 in the spinal cord in paclitaxel-induced mechanical allodynia. Mol Pain, 2014;10(0):53. 2014 PMID: 25127716
L Janks, CVR Sharma, TM Egan A central role for P2X7 receptors in human microglia J Neuroinflammation, 2018;15(1):325. 2018 PMID: 30463629
BH Hinrichs, JD Matthews, D Siuda, MN O'Leary, AA Wolfarth, BJ Saeedi, A Nusrat, AS Neish Serum Amyloid A1 is an epithelial pro-restitutive factor Am. J. Pathol., 2018;0(0):. 2018 PMID: 29366677
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(2):353-9. 2012 PMID: 22706314
Nelson et al. Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X₇ antagonists. J.Med.Chem., 2006;49:3659 PMID: 16759108
Donnelly-Roberts and Jarvis Discovery of P2X₇ receptor-selective antagonists offers new insights into P2X₇ receptor function and indicates a role in chronic pain states. Br.J.Pharmacol., 2007;151:571 PMID: 17471177
McGaraughty et al. P2X₇-related modulation of pathological nociception in rats. Neuroscience, 2007;146:1817 PMID: 17478048
Fernandes et al. Methamphetamine alters microglial immune function through P2X₇R signaling. J.Neuroinflammation., 2016;13:91 PMID: 27117066