p2x7r

AZ10606120 dihydrochloride is a selectable, potent, high-affinity receptor antagonist with K D values of 1.4 and 19 nM at human and rat P2X 7 receptors, respectively. AZ10606120 dihydrochloride inhibits tumor growth and has anti-angiogenic activity. AZ 10606120 acts as a negative allosteric modulator when bound to a site coupled to the ATP binding site.

A-804598 is a competitive and selective P2X7 receptor antagonist (IC50: 10 nM, rat; 9 nM, mouse; 11 nM, human).

P2X7 receptor antagonist-3 is a potent inhibitor of the P2X7 receptor, with IC50 values of 4.2 nM in humans and 6.8 nM in rats, demonstrating its high efficacy across species.

Oxidized ATP trisodium salt (oATP) is a broad-spectrum P2 receptor inhibitor that irreversibly antagonizes P2X7R activation and inhibits CRP-induced NLRP3 inflammasome activation, making it useful in atherosclerosis research [1] [2].

Compound 14a (P2X7 receptor antagonist-4) is a P2X7R antagonist with IC50 values of 64.7 nM in humans and 10.1 nM in mice. It inhibits the activation of the NLRP3 inflammasome, which subsequently reduces the expression of caspase-1, gasdermin D, IL-1β, and IL-18 in the kidneys of mice with sepsis-induced damage [1].

HEI3090 is an activator of the P2X7R receptor. This compound enhances the production of IL-18 by stimulating dendritic cells that express P2X7R, which in turn promotes the production of IFN-γ by natural killer cells and CD4T cells within tumors, triggering a sustained anti-tumor response. Additionally, HEI3090 can be used to improve the efficacy of αPD-1 therapy in non-small cell lung cancer (NSCLC).