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A-740003

Chemical Structure : A-740003

CAS No.: 861393-28-4

A-740003 (A 740003;A740003)

Catalog No.: PC-45846Not For Human Use, Lab Use Only.

A-740003 (A740003) is a potent, selective, competitive P2X7 receptor antagonist with IC50 of 40 nM and 18 nM for hP2X7 and rP2X7, respectively.

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Biological Activity

A-740003 (A740003) is a potent, selective, competitive P2X7 receptor antagonist with IC50 of 40 nM and 18 nM for hP2X7 and rP2X7, respectively; showed weak or no activity for other P2 receptors (IC50>10 uM); potently blocks agonist-evoked IL-1β release (IC50=156 nM) and pore formation (IC50=92 nM) in differentiated human THP-1 cells; produces dose-dependent antinociception in a spinal nerve ligation model (ED50=19 mg/kg i.p.) in the rat.

Pain

Discontinued

Physicochemical Properties

M.Wt 474.5548
Formula C26H30N6O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Benzeneacetamide, N-[1-[[(cyanoamino)(5-quinolinylimino)methyl]amino]-2,2-dimethylpropyl]-3,4-dimethoxy-

References

1. Honore P, et al. J Pharmacol Exp Ther. 2006 Dec;319(3):1376-85.

2. Morytko MJ, et al. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2093-6.

3. King BF. Br J Pharmacol. 2007 Jul;151(5):565-7.

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