TLR7 agonist22 (Compound 11a) is a selective TLR7 agonist with an IC50 value of 25.86 μM. It inhibits the secretion of cell HBsAg and effectively activates TLR7, inducing the release of TLR7-regulated cytokines IL-12, TNF-α, and IFN-α in human PBMC cells. TLR7 agonist22 shows promise for developing novel immunomodulatory drugs in HBV research.

HBV DNA:25.86 μM

TLR7 agonist 22 inhibits HBV DNA replication in HepG2 cells at a concentration of 4 μM over 72 hours, with an IC50 value of 0.36 μM. It demonstrates TLR7 agonistic effects by significantly enhancing TLR7-induced NF-κB activity at concentrations of 0.4, 2, and 10 μM over 48 hours. Additionally, TLR7 agonist 22 dose-dependently increases the production of IL-12, TNF-α, and IFN-α in human PBMC cells at concentrations of 0.4, 2, and 10 μM over 24 hours.

The TLR7 agonist 22 (10 MG/KG, i.g.) demonstrates a relatively suitable absorption and elimination timeframe in male Sprague-Dawley rats.