A selective P2X7 antagonist
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A-740003

Item No. 21256

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[1-[[(cyanoamino)(5-quinolinylimino)methyl]amino]-2,2-dimethylpropyl]-3,4-dimethoxy-benzeneacetamide
CAS Number
861393-28-4
Molecular Formula
C26H30N6O3
Formula Weight
474.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/mlDMSO:PBS(pH 7.2) (1:4): 0.2 mg/ml
λmax
226, 282 nm
SMILES
COC1=CC=C(CC(NC(C(C)(C)C)N/C(NC#N)=N\C2=C(C=CC=N3)C3=CC=C2)=O)C=C1OC
InChi Code
InChI=1S/C26H30N6O3/c1-26(2,3)24(31-23(33)15-17-11-12-21(34-4)22(14-17)35-5)32-25(29-16-27)30-20-10-6-9-19-18(20)8-7-13-28-19/h6-14,24H,15H2,1-5H3,(H,31,33)(H2,29,30,32)
InChi Key
PUHSRMSFDASMAE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Cayman Chemical
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    Product Description

    A-740003 is a competitive antagonist of the ATP-gated ionotropic P2X7 receptor (IC50s = 40 and 18 nM for human and rat receptors, respectively).1 It shows weak or no activity at other P2 receptors and other receptors and ion channels. A-740003 blocks agonist-induced IL-1β release and pore formation in differentiated THP-1 cells (IC50s = 156 and 92 nM, respectively).1 It is effective in vivo when administered intraperitoneally, reducing pain in several animal models.1 A-740003 is used in cell and animal studies to elucidate P2X7 roles and signaling pathways.2,3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Honore, P., Donnelly-Roberts, D., Namovic, M.T., 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. 319(3), 1376-1385 (2006).

    2. Donnelly-Roberts, D.L., and Jarvis, M.F. Discovery of P2X7 receptor-selective antagonists offers new insights into P2X7 receptor function and indicates a role in chronic pain states. Br. J. Pharmacol. 151(5), 571-579 (2007).

    3. Gicquel, T., Robert, S., Loyer, P., et al. IL-1β production is dependent on the activation of purinergic receptors and NLRP3 pathway in human macrophages. The FASEB Journal 29(10), 4162-4173 (2015).

    4. Grol, M.W., Brooks, P.J., Pereverzev, A., et al. P2X7 nucleotide receptor signaling potentiates the Wnt/β-catenin pathway in cells of the osteoblast lineage. Purinergic Signal. 12(3), 509-520 (2016).