TLR7/8 agonist 13
TLR7/8 agonist 13 is an orally active dual agonist of TLR7 (lowest effective concentrations (LEC) [hTLR7] = 1.6 μM) and TLR8 (LEC [hTLR8] = 1.6 μM). TLR7/8 agonist 13 exhibits agonistic activity against human peripheral blood mononuclear cells (hPBMCs) (LEC [hPBMC] = 0.5 μM). TLR7/8 agonist 13 induces endogenous IFNα, activating myeloid dendritic cells and monocytes toward a TH1 phenotype in mice and cynomolgus monkeys. TLR7/8 agonist 13 reduces viral load and HBV surface antigen expression in a mouse model of chronic AAV-HBV infection. TLR7/8 agonist 13 has the potential to indirectly induce IFNγ, which may promote HBV antigen-specific CD8 T cell-mediated responses. TLR7/8 agonist 13 can be used to study hepatitis B virus.
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- CAS No.: 1402802-45-2
- Formule: C12H22N4O2
- Masse moléculaire:254.33
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Help & FAQs
Activité biologique
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human TLR7 |
TLR8 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | CC50 |
>24 μM
Compound: 50d
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Cytotoxicity against HEK293 cells measured after 6 hrs
Cytotoxicity against HEK293 cells measured after 6 hrs
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[PMID: 27513093] |
TLR7/8 agonist 13 (Compound 50 d) induces IFNα, IFNγ, IL-12p40, IL-12p70, and TNF-α production in PBMCs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Cmax | Tmax |
|---|---|---|---|---|
| Rat[1] | 10 mg/kg | p.o. | 65 ng/mL | 1 h |
TLR7/8 agonist 13 (5 mg/kg, p.o., once a week, 8 weeks) inhibits HBsAg secretion and HBV viral load by two distinct noncytotoxic mechanisms in AAV-HBV C57Bl/6 mice model[1].
TLR7/8 agonist 13 (3-30 mg/kg, p.o., once) induces endogenous IFNα, an interferon stimulated gene response, but also activation of myeloid dendritic cells and monocytes toward a TH1 phenotype in cynomolgus monkeys model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57Bl/6 mice model[1]
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Dosage:1, 5, 10, and 50 mg/kg
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Administration:p.o. once
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Result:Induced IFNα at low dose as well as TH1 and myeloid responses at higher doses.
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Animal Model:AAV-HBV C57Bl/6 mice model[1]
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Dosage:5 mg/kg
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Administration:p.o., once a week, 8 weeks
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Result:Decreased HBsAg levels by 2.4 log at the end of the dosing period, decreased the percent of HBsAg hepatocytes, decreased HBV viral load in the serum, had no decrease in liver HBV RNA levels nor in the percent of HBcAg hepatocytes.
Increased serum anti-HBsAg antibody levels.
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Animal Model:Cynomolgus monkeys model[1]
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Dosage:3, 9, and 30 mg/kg
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Administration:p.o., once
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Result:Had no change of clinical observations and body weight, body temperature, clinical pathology.
Induced IFNα production from the 9 mg/kg dose, induced an ISG response and CXCL10 from a lower dose than IFNα, i.e., 3 mg/kg.
Up-regulated Isg15 and Mx1, activated monocytes, IL-15 from 9 mg/kg, activated Myeloid dendritic cells, MCP1, MIP-1β, and IL-1Ra from 3 to 9 mg/kg, activated TNFα and IL-6 from 30 mg/kg.
Chemical Information
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CAS No. 1402802-45-2
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Masse moléculaire 254.33
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Formule C12H22N4O2
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SMILES
NC(N=C1N[C@H](CCO)CCCC)=NC=C1OC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TLR7/8 agonist 13 Related Classifications
HY-177300 Related Classifications
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