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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.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| 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 |
| Smiles | N([C@@H](CCCC)CCO)C=1C(OC)=CN=C(N)N1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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