A-740003 - CAS 861393-28-4
Catalog number: 861393-28-4
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
P2X Receptor
A-740003 is potent, selective and competitive P2X7 receptor antagonist. Its IC50 values are 18 and 40 nM for rat and human receptors respectively measured by agonist-stimulated changes in intracellular calcium concentrations. It displays selectivity over a variety of P2X and P2Y receptors up to a concentration of 100 μM. It reduces nociception in animal models of persistent neuropathic and inflammatory pain. It showed weak or no activity (IC(50) > 10 muM) at other P2 receptors and an array of other neurotransmitter and peptide receptors, ion channels, reuptake sites, and enzymes. It potently blocked agonist-evoked IL-1beta release (IC(50) = 156 nM) and pore formation (IC(50) = 92 nM) in differentiated human THP-1 cells. It produces significant antinociception in animal models of neuropathic and inflammatory pain in vivo.
>98 %
Solid powder
N-[1-[[(Cyanoamino)(5-quinolinylimino)methyl]amino]-2,2-dimethylpropyl]-3,4-dimethoxybenzeneacetamide;N-(1-{[(cyanoimino)(5-quinolinylamino) methyl] amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide
20 mM in DMSO
-20°C Freezer
A-740003 produces significant antinociception in animal models of neuropathic and inflammatory pain in vivo.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Melting Point:
128-129 °C
1.19±0.1 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
Canonical SMILES:
1.Trophic activity of human P2X7 receptor isoforms A and B in osteosarcoma.
Giuliani AL;Colognesi D;Ricco T;Roncato C;Capece M;Amoroso F;Wang QG;De Marchi E;Gartland A;Di Virgilio F;Adinolfi E PLoS One. 2014 Sep 16;9(9):e107224. doi: 10.1371/journal.pone.0107224. eCollection 2014.
The P2X7 receptor (P2X7R) is attracting increasing attention for its involvement in cancer. Several recent studies have shown a crucial role of P2X7R in tumour cell growth, angiogenesis and invasiveness. In this study, we investigated the role of the two known human P2X7R functional splice variants, the full length P2X7RA and the truncated P2X7RB, in osteosarcoma cell growth. Immunohistochemical analysis of a tissue array of human osteosarcomas showed that forty-four, of a total fifty-four tumours (81.4%), stained positive for both P2X7RA and B, thirty-one (57.4%) were positive using an anti-P2X7RA antibody, whereas fifteen of the total number (27.7%) expressed only P2X7RB. P2X7RB positive tumours showed increased cell density, at the expense of extracellular matrix. The human osteosarcoma cell line Te85, which lacks endogenous P2X7R expression, was stably transfected with either P2X7RA, P2X7RB, or both. Receptor expression was a powerful stimulus for cell growth, the most efficient growth-promoting isoform being P2X7RB alone. Growth stimulation was matched by increased Ca(2+) mobilization and enhanced NFATc1 activity. Te85 P2X7RA+B cells presented pore formation as well as spontaneous extracellular ATP release.
2.The P2X7 Receptor Primes IL-1β and the NLRP3 Inflammasome in Astrocytes Exposed to Mechanical Strain.
Albalawi F;Lu W;Beckel JM;Lim JC;McCaughey SA;Mitchell CH Front Cell Neurosci. 2017 Aug 8;11:227. doi: 10.3389/fncel.2017.00227. eCollection 2017.
Inflammatory responses play a key role in many neural pathologies, with localized signaling from the non-immune cells making critical contributions. The NLRP3 inflammasome is an important component of innate immune signaling and can link neural insult to chronic inflammation. The NLRP3 inflammasome requires two stages to contribute: priming and activation. The priming stage involves upregulation of inflammasome components while the activation stage results in the assembly and activation of the inflammasome complex. The priming step can be rate limiting and can connect insult to chronic inflammation, but our knowledge of the signals that regulate NLRP3 inflammasome priming in sterile inflammation is limited. This study examined the link between mechanical strain and inflammasome priming in neural systems. Transient non-ischemic elevation of intraocular pressure increased mRNA for inflammasome components ;IL-1;β;, NLRP3, ASC;, and ;CASP1; in rat and mouse retinas. The elevation was greater 1 day after the insult, with the rise in IL-1β most pronounced. The P2X7 receptor was implicated in the mechanosensitive priming of IL-1β mRNA ;in vivo;, as the antagonist Brilliant Blue G (BBG) blocked the increased expression, the agonist BzATP mimicked the pressure-dependent rise in IL-1β, and the rise was absent in P2X7 knockout mice.
3.p38 MAPK mediates glial P2X7R-neuronal P2Y1R inhibitory control of P2X3R expression in dorsal root ganglion neurons.
Chen Y;Li G;Huang LY Mol Pain. 2015 Nov 5;11:68. doi: 10.1186/s12990-015-0073-7.
BACKGROUND: ;We have previously shown that endogenously active purinergic P2X7 receptors (P2X7Rs) in satellite glial cells of dorsal root ganglia (DRGs) stimulate ATP release. The ATP activates P2Y1Rs located in the enwrapped neuronal somata, resulting in down-regulation of P2X3Rs. This P2X7R-P2Y1-P2X3R inhibitory control significantly reduces P2X3R-mediated nociceptive responses. The underlying mechanism by which the activation of P2Y1Rs inhibits the expression of P2X3Rs remains unexplored.;RESULTS: ;Examining the effect of the activation of p38 mitogen-activated protein kinase on the expression of P2X3Rs in DRGs, we found that the p38 activator, anisomycin (Anis), reduced the expression of P2X3Rs. Blocking the activity of SGCs by the glial Krebs cycle inhibitor, fluorocitrate, did not change the effect of Anis. These results suggest that neuronal p38 plays a major role in the inhibition of P2X3R expression. Western blotting analyses showed that inhibiting P2Y1Rs by MRS2179 (MRS) or blocking P2X7Rs by either oxATP or A740003 reduced pp38 and increased P2X3R expression in DRGs. These results are further supported by the immunohistochemical study showing that P2X7R and P2Y1R antagonists reduce the percentage of pp38-positive neurons.
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CAS 861393-28-4 A-740003

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