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TLR7/8 agonist 13 is an orally active dual agonist of TLR7 (with a lowest effective concentration (LEC) [hTLR7] of 1.6 μM) and TLR8 (LEC [hTLR8] of 1.6 μM). It acts on human peripheral blood mononuclear cells (hPBMC) with agonistic activity (LEC [hPBMC] = 0.5 μM). In mice and cynomolgus monkeys, TLR7/8 agonist 13 induces endogenous IFNα, activates myeloid dendritic cells and monocytes, promoting their differentiation towards a TH1 phenotype. In chronic AAV-HBV mouse models, it reduces viral load and HBV surface antigen levels. TLR7/8 agonist 13 has the potential to indirectly induce IFNγ, facilitating the response of HBV antigen-specific CD8 T cells. This compound is useful for hepatitis B virus research.


| Description | TLR7/8 agonist 13 is an orally active dual agonist of TLR7 (with a lowest effective concentration (LEC) [hTLR7] of 1.6 μM) and TLR8 (LEC [hTLR8] of 1.6 μM). It acts on human peripheral blood mononuclear cells (hPBMC) with agonistic activity (LEC [hPBMC] = 0.5 μM). In mice and cynomolgus monkeys, TLR7/8 agonist 13 induces endogenous IFNα, activates myeloid dendritic cells and monocytes, promoting their differentiation towards a TH1 phenotype. In chronic AAV-HBV mouse models, it reduces viral load and HBV surface antigen levels. TLR7/8 agonist 13 has the potential to indirectly induce IFNγ, facilitating the response of HBV antigen-specific CD8 T cells. This compound is useful for hepatitis B virus research. |
| In vitro | TLR7/8 agonist 13 (Compound 50 d) stimulates PBMCs to produce IFNα, IFNγ, IL-12p40, IL-12p70, and TNF-α. |
| In vivo | In a C57Bl/6 mouse model, TLR7/8 agonist 13 (Compound 50 d) (1-50 mg/kg, oral, single dose) induces the response of IFNα, TH1, and myeloid cells. Administered at 5 mg/kg orally once a week for 8 weeks, it inhibits the secretion of HBsAg and reduces HBV viral load through two non-cytotoxic mechanisms in the AAV-HBV C57Bl/6 mouse model. In crab-eating macaques, TLR7/8 agonist 13 (3-30 mg/kg, oral, single dose) stimulates endogenous IFNα production and activates myeloid dendritic cells and monocytes, promoting their development into a TH1 phenotype. |
| Molecular Weight | 254.33 |
| Formula | C12H22N4O2 |
| Cas No. | 1402802-45-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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