Date published: 2026-1-31

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A 740003 (CAS 861393-28-4)

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Alternate Names:
N-[1-[[(Cyanoamino)(5-quinolinylamino)methylene]amino]- 2,2-dimethylpropyl]-3,4-dimethoxybenzeneacetamide
Application:
A 740003 is a potent, selective and competitive P2X7 receptor antagonist
CAS Number:
861393-28-4
Purity:
≥98%
Molecular Weight:
474.56
Molecular Formula:
C26H30N6O3
Supplemental Information:
This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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A 740003 is a competitive antagonist of P2X7 receptors that may act to potently block proinflammatory cytokine interleukin-1beta (IL-1beta) release. Experiments have reported that a slight activation of P2X7 receptors causes a rapid increase in the opening of non-selective cation channels. P2X7 receptors are ATP-sensitive and localized on cells of immunological origin.


A 740003 (CAS 861393-28-4) References

  1. 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.  |  Honore, P., et al. 2006. J Pharmacol Exp Ther. 319: 1376-85. PMID: 16982702
  2. Novel P2X7 receptor antagonists ease the pain.  |  King, BF. 2007. Br J Pharmacol. 151: 565-7. PMID: 17471176
  3. Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors.  |  Donnelly-Roberts, DL., et al. 2009. Br J Pharmacol. 157: 1203-14. PMID: 19558545
  4. P2X₇-mediated calcium influx triggers a sustained, PI3K-dependent increase in metabolic acid production by osteoblast-like cells.  |  Grol, MW., et al. 2012. Am J Physiol Endocrinol Metab. 302: E561-75. PMID: 22185840
  5. Synthesis and initial preclinical evaluation of the P2X7 receptor antagonist [¹¹C]A-740003 as a novel tracer of neuroinflammation.  |  Janssen, B., et al. 2014. J Labelled Comp Radiopharm. 57: 509-16. PMID: 24995673
  6. Activation of P2X7 receptors in the midbrain periaqueductal gray of rats facilitates morphine tolerance.  |  Xiao, Z., et al. 2015. Pharmacol Biochem Behav. 135: 145-53. PMID: 26054441
  7. Role of P2X7R in the development and progression of pulmonary hypertension.  |  Yin, J., et al. 2017. Respir Res. 18: 127. PMID: 28646872
  8. A cyclic pathway of P2 × 7, bradykinin, and dopamine receptor activation induces a sustained articular hyperalgesia in the knee joint of rats.  |  Teixeira, JM., et al. 2018. Inflamm Res. 67: 301-314. PMID: 29260240
  9. Activation of the P2X7 receptor in midbrain periaqueductal gray participates in the analgesic effect of tramadol in bone cancer pain rats.  |  Li, P., et al. 2018. Mol Pain. 14: 1744806918803039. PMID: 30198382
  10. Activation of the P2X7 receptor in the dental pulp tissue contributes to the pain in rats with acute pulpitis.  |  Xiao, Z., et al. 2022. Mol Pain. 18: 17448069221106844. PMID: 35748325
  11. ATP ion channel P2X purinergic receptors in inflammation response.  |  Liu, JP., et al. 2023. Biomed Pharmacother. 158: 114205. PMID: 36916431
  12. P2X and P2Y receptor antagonists reduce inflammation in ATP-induced microglia.  |  Imraish, A., et al. 2023. Pharm Pract (Granada). 21: 2788. PMID: 37090457

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

A 740003, 10 mg

sc-291774
10 mg
$176.00

A 740003, 50 mg

sc-291774A
50 mg
$733.00