A 740003

Name: A 740003
Brand: Tocris Bioscience
SKU: 3701

Tocris Bioscience, part of Bio-Techne | Catalog # 3701

Citations (90)

COA / SDS

Potent and selective P2X7 antagonist

Key Product Details

Chemical Name:	N-[1-[[(Cyanoamino)(5-quinolinylamino)methylene]amino]-2,2-dimethylpropyl]-3,4-dimethoxybenzeneacetamide
Purity:	≥97%
Molecular Weight:	474.55 kDa

View Full Technical Details for A 740003

Technical Data
Citations

Biological Activity for A 740003

A 740003 is a potent and selective P2X₇ receptor antagonist (IC₅₀ values are 18 and 40 nM for rat and human receptors respectively). Displays selectivity over a variety of P2X and P2Y receptors up to a concentration of 100 μM. Reduces nociception in animal models of persistent neuropathic and inflammatory pain. Also reduces neuroblastoma tumor growth in mice.

Technical Data for A 740003

M. Wt	474.55 kDa
Formula	C₂₆H₃₀N₆O₃
Storage	Store at +4°C
Purity	≥97%
CAS Number	861393-28-4

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 740003

Solubility

Soluble Soluble to 20 mM in DMSO

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References for A 740003

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

M Lombardi, ME Mantione, D Baccellier, D Ferrara, R Castellano, R Chiesa, O Alfieri, C Foglieni P2X7 receptor antagonism modulates IL-1? and MMP9 in human atherosclerotic vessels Sci Rep, 2017;7(1):4872. 2017 PMID: 28687781
F Albalawi, W Lu, JM Beckel, JC Lim, SA McCaughey, CH Mitchell The P2X7 Receptor Primes IL-1? and the NLRP3 Inflammasome in Astrocytes Exposed to Mechanical Strain Front Cell Neurosci, 2017;11(0):227. 2017 PMID: 28848393
X Wu, J Ren, G Chen, L Wu, X Song, G Li, Y Deng, G Wang, G Gu, J Li Systemic blockade of P2X7 receptor protects against sepsis-induced intestinal barrier disruption Sci Rep, 2017;7(1):4364. 2017 PMID: 28663567
Luheshi NM, Giles JA, Lopez-Castejon G, Brough D Sphingosine regulates the NLRP3-inflammasome and IL-1beta release from macrophages. Eur. J. Immunol., 2011;42(3):716-25. 2011 PMID: 22105559
Hazleton JE, Berman JW, Eugenin EA Purinergic receptors are required for HIV-1 infection of primary human macrophages. J. Immunol., 2012;188(9):4488-95. 2012 PMID: 22450808
Adinolfi E, Capece M, Franceschini A, Falzoni S, Giuliani A, Rotondo A, Sarti A, Bonora M, Syberg S, Corigliano D, Pinton P, Jorgensen N, Abelli L, Emionite L, Raffaghello L, Pistoia V, Di Virgilio F Accelerated tumor progression in mice lacking the ATP receptor P2X7. Cancer Res, 2015;75(4):635-44. 2015 PMID: 25542861
Cláudia Herrera Tambeli Intra-articular blockade of P2X7 receptor reduces the articular hyperalgesia and inflammation in the knee joint synovitis especially in female rats J Pain, 2016;0(0):. 2016 PMID: 27818192
Honore et al. A-740003 [N-(1-{[(cyanoimino)(5-quinolinylamino)methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide], a novel and selective P2X₇ receptor antagonist, dose-dependently reduces neuropathic pain in the rat. J.Pharmacol.Exp.Ther., 2006;319:1376 PMID: 16982702
King Novel P2X₇ receptor antagonists ease the pain. Br.J.Pharmacol., 2007;151:565 PMID: 17471176
Donnelly-Roberts et al. Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors. Br.J.Pharmacol., 2009;157:1203 PMID: 19558545
Amoroso et al. The P2X7 receptor is a key modulator of the PI3K/GSK3β/VEGF signaling network: evidence in experimental neuroblastoma. Oncogene, 2015;34:5240 PMID: 25619831