TLR7/8 agonist 1 is a dual agonist of toll-like receptor 7 (TLR7) and TLR8 (EC50s = 50 and 55 nM, respectively, in cell-based assays).1 It increases the levels of TNF-α, IFN-γ, IL-12p40, and chemokine (C-C motif) ligand 4 (CCL4) in human peripheral blood mononuclear cells (PBMCs) in a biphasic manner. TLR7/8 agonist 1 (25 nmol, s.c.) increases serum levels of IL-12p40 and chemokine (C-X-C motif) ligand 10 (CXCL10), as well as the number of dendritic cells per injection-site proximal lymph node, in mice.2 It has been conjugated to various fluorophores as TLR7 probes and to polymer particles for the modulation of TLR7/8 agonist 1 adjuvant activity.3,2
1.Beesu, M., Caruso, G., Salyer, A.C., et al.Structure-based design of human TLR8-specific agonists with augmented potency and adjuvanticityJ. Med. Chem.58(19)7833-7849(2015) 2.Lynn, G.M., Chytil, P., Francica, J.R., et al.Impact of polymer-TLR-7/8 agonist (adjuvant) morphology on the potency and mechanism of CD8 T cell inductionBiomacromolecules20(2)854-870(2019) 3.Shukla, N.M., Mutz, C.A., Ukani, R., et al.Syntheses of fluorescent imidazoquinoline conjugates as probes of Toll-like receptor 7Bioorg. Med. Chem. Lett.20(22)6384-6386(2010)