AZ 11645373 

AZ11645373 is a highly selective and potent antagonist at human but not rat P2X7 receptors，AZ11645373 inhibits ATP-evoked IL-1β release from lipopolysaccharide-activated THP-1 cells , with an IC₅₀ value of 90 nM^[1].

AZ11645373 produces a concentration-dependent inhibition of BzATP-mediated calcium transients, with complete inhibition observed at concentrations between 100 and 300 nM according to concentration-inhibition curves^[1].
AZ11645373 inhibits ATP- or BzATP-evoked YO-PRO1 fluorescence in HEK cells stably expressing hP2X7R, but not in cells expressing rP2X7R, with an K_B value not significantly different from those obtained in experiments measuring membrane currents or calcium mobilization^[1].
AZ11645373 (0.01, 0.1, 1 μM; 30 min) has no significant effect on basal levels of IL-1β in culture medium of LPS-treated cells, but produces a concentration-dependent inhibition of ATP-mediated IL-1β release with a calculated K_B value of 92 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

463.51

C₂₄H₂₁N₃O₅S

227088-94-0

O=C(N1C(COC2=CC=C(C3=CC=CC([N+]([O-])=O)=C3)C=C2)CCC4=CC=NC=C4)SCC1=O

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• [1]. Stokes L, et al. Characterization of a selective and potent antagonist of human P2X(7) receptors, AZ11645373. Br J Pharmacol. 2006 Dec;149(7):880-7.  [Content Brief]