A-740003

A-740003 is a competitive antagonist of the ATP-gated ionotropic P2X7 receptor (IC50s = 40 and 18 nM for human and rat receptors, respectively). It shows weak or no activity at other P2 receptors and other receptors and ion channels. A-740003 blocks agonist-induced IL-1beta release and pore formation in differentiated THP-1 cells (IC50s = 156 and 92 nM, respectively). It is effective in vivo when administered intraperitoneally, reducing pain in several animal models. A-740003 is used in cell and animal studies to elucidate P2X7 roles and signaling pathways.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: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMSO: 1 mg/ml, DMSO:PBS(pH 7.2) (1:4): 0.2 mg/ml. lambdamax: 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.