A740003 inhibited the activation of NLRP3 inflammasome and phosphorylation of IKBα and decreased the expression of P2X7R in ARPE-19 cells exposed to ox-LDL for 24 hours. ELISA results showed that A740003 pretreatment decreased the secretion of inflammatory cytokines including IL-1β (to 2.831 ± 0.1162) (a) and IL-18 (to 1.585 ± 0.2329) (b) significantly. Besides, compared to the vehicle-treated group, A740003 pretreatment significantly inhibited NLRP3 (56.73% ± 0.3908) (c) and P2X7R (51.30% ± 0.1196) (d) at mRNA levels in ARPE-19 cells. It indicated that A740003 inhibited the overexpression of P2X7R and NLRP3 which was induced by ox-LDL. Western blot showed that A740003 downregulated the protein levels of NLRP3 (64.92% ± 0.1264) (e, g), pro-Caspase-1 (68.26% ± 0.02456) (f, j), Caspase-1 (65.97% ± 0.01661) (f, k), and P2X7R (60.55% ± 0.09754) (e, h) and the phosphorylation of IKBα (79.34% ± 0.01995) (e, i) significantly compared to the vehicle-treated group. Symbols: +: with; −: without. The results were mean ± SEM. Significance of difference (∗p < 0.05, ∗∗p < 0.01, and ∗∗∗p < 0.001) was determined by using one-way ANOVA with Bonferroni correction.