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Chemical Structure : A-740003
CAS No.: 861393-28-4
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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A-740003 (A740003) is a potent, selective, competitive P2X7 receptor antagonist with IC50 of 40 nM and 18 nM for hP2X7 and rP2X7, respectively.
A-740003 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.
A-740003 produces dose-dependent antinociception in a spinal nerve ligation model (ED50=19 mg/kg i.p.) in the rat.
| M.Wt | 474.5548 | |
| Formula | C26H30N6O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
Benzeneacetamide, N-[1-[[(cyanoamino)(5-quinolinylimino)methyl]amino]-2,2-dimethylpropyl]-3,4-dimethoxy- |
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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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