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A-740003

Catalog No. T3690 CAS 861393-28-4

Synonyms: A 740003

A-740003 (A 740003) is an effective and specific P2X7 receptor antagonist (IC50: 18/40 nM, for rat/human). It can reduce nociception in animal models of persistent neuropathic and inflammatory pain, and also reduce neuroblastoma tumor growth in mice.

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A-740003, CAS 861393-28-4

Pack Size	Availability	Price/USD
5 mg	In stock	$ 34.00
10 mg	In stock	$ 53.00
50 mg	In stock	$ 72.00
100 mg	In stock	$ 114.00

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Purity: 99.51%

Purity: 96.53%

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Description	A-740003 (A 740003) is an effective and specific P2X7 receptor antagonist (IC50: 18/40 nM, for rat/human). It can reduce nociception in animal models of persistent neuropathic and inflammatory pain, and also reduce neuroblastoma tumor growth in mice.
Targets&IC50	P2X7 (rat):18nM, P2X7 (human):40 nM
In vitro	A-438079 and A-740003 (10 μM) effectively inhibit the prolonged phase of BzATP-induced responses[1] and mitigate SE-induced TNF-α expression in dentate granule neurons while increasing SE-induced neuronal death[2]. Compared to other antagonists, both compounds exhibit superior efficacy in inhibiting P2X7 receptor activation across various species, with heightened activity in rat and human compared to mouse P2X7 receptors[3]. Specifically, A-740003 robustly inhibits agonist-induced IL-1β release (IC50=156 nM) and pore formation (IC50=92 nM) in differentiated human THP-1 cells[4].
In vivo	Administering A-740003 systemically results in a dose-dependent reduction of pain (antinociception) in rats, as evidenced in a spinal nerve ligation model (ED50=19 mg/kg i.p.), indicating its potency. Furthermore, A-740003 diminishes sensitivity to touch (tactile allodynia) in models of neuropathic pain, including chronic constriction of the sciatic nerve and vincristine-induced neuropathy. It also significantly lowers increased sensitivity to heat (thermal hyperalgesia) following the intraplantar introduction of carrageenan or complete Freund's adjuvant (ED50=38-54 mg/kg i.p.). However, A-740003 does not affect acute thermal pain in healthy rats and does not impair motor skills at doses that relieve pain.

Synonyms	A 740003
Molecular Weight	474.55
Formula	C26H30N6O3
CAS No.	861393-28-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 9.5 mg/mL(20 mM)

References and Literature

1. Kim, J., Ryu, H., & Kang, T. (2011). P2X7 receptor activation ameliorates CA3 neuronal damage via a tumor necrosis factor-α-mediated pathway in the rat hippocampus following status epilepticus. Journal Of Neuroinflammation, 8(1), 62. doi: 10.1186/1742-2094-8-62 2. Donnelly-Roberts DL, et al. Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors.Br J Pharmacol. 2009 Aug;157(7):1203-14. Epub 2009 Jun 22. 3. Honore P, et al. A-74202003 [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 Th 4. Tian C, Han X, He L, et al. Transient receptor potential ankyrin 1 contributes to the ATP-elicited oxidative stress and inflammation in THP-1-derived macrophage[J]. Molecular and Cellular Biochemistry. 2020: 1-14.

Citations

1. Xiao Z, Xu M, Lan L, et al. Activation of the P2X7 receptor in the dental pulp tissue contributes to the pain in rats with acute pulpitis. Molecular Pain. 2022, 18: 17448069221106844 2. Tian C, Han X, He L, et al. Transient receptor potential ankyrin 1 contributes to the ATP-elicited oxidative stress and inflammation in THP-1-derived macrophage. Molecular and Cellular Biochemistry. 2020: 1-14

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Anti-Neurodegenerative Disease Compound Library Preclinical Compound Library Bioactive Compound Library NO PAINS Compound Library Ion Channel Inhibitor Library Neuronal Signaling Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library

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Keywords

A-740003 861393-28-4 Membrane transporter/Ion channel Neuroscience P2X Receptor P2XRs inhibit A 740003 Inhibitor A740003 inhibitor

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