Resiquimod [144875-48-9]

Resiquimod (R848) is an agonist of Toll-like receptors 7 and 8 (TLR7/TLR8) that induces the upregulation of cytokines including TNF-α, IL-6, and IFN-α. It possesses immunomodulatory, antitumor, and antiviral activities, and can be used to induce models of myocarditis and systemic lupus erythematosus (SLE).

TLR7:1.5 ± 0.3 μM (EC50), TLR8:4.5 ± 3.2 μM (EC50)

METHODS: Golden pompholyte kidney lymphocytes HKL were treated with Resiquimod (0.175-32 µg/mL) for 12 h. Cell viability was measured by CCK8 assay.
RESULTS: CCK8 assay showed that 0.25-32 µg/mL Resiquimod significantly promoted HKL proliferation. [1]
METHODS: Peripheral blood mononuclear cells PBM were treated with Resiquimod (0.01-100 µM) for 1-14 h, and the expression levels of target proteins were detected by Western Blot.
RESULTS: A dose of 1 µM was sufficient to alter the expression of FcγR, and higher doses did not result in greater changes. the increase in FcγRIIa occurred at a late stage, while a small increase in the γ chain was seen at 3 h, but was higher at 14 h. However, the FcγRIIb protein decreases at 1 h, while the FcγRIIb transcript is maintained until 4 h.[2]

METHODS: To detect anti-tumor activity in vivo, Resiquimod (2 mg/kg) and 4D5 anti-HER2 antibody (20 mg/kg) were injected intraperitoneally three times per week for 13 days into Balb/cJ mice bearing CT26-HER2/neu tumors.
RESULTS: After 13 days, the tumor growth rate of mice receiving Resiquimod plus antibody was significantly reduced. Statistical tests showed a synergistic effect of 4D5 and Resiquimod in reducin