P2X7 receptor antagonist-4 (Compound 14a) is a P2X7R antagonist. The P2X7 receptor antagonist-4 values of P2X7R IC50 in human and mouse are 64.7 and 10.1 nM, respectively. P2X7 receptor antagonist-4 can inhibit the activation of NLRP3 inflammasome, thereby inhibiting the expression of caspase-1, gasdermin D, IL-1β and IL-18 in the damaged kidney of sepsis mice.
References:
[1]. Zhang R, et al. Design, Synthesis, and Biological Evaluation of Novel P2X7 Receptor Antagonists for the Treatment of Septic Acute Kidney Injury. J Med Chem. 2023 Aug 24;66(16):11365-11389.
















