2. Immunology/Inflammation Anti-infection
  3. Toll-like Receptor (TLR) HBV IFNAR Interleukin Related
  4. 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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TLR7/8 agonist 13

TLR7/8 agonist 13 Chemical Structure

CAS No. : 1402802-45-2

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TLR7/8 agonist 13 Related Antibodies

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Description

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[1].

IC50 & Target[1]

human TLR7

 

TLR8

 

In Vitro

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.

TLR7/8 agonist 13 Related Antibodies
In Vivo

TLR7/8 agonist 13 (Compound 50 d) (1-50 mg/kg, p.o. once) induces IFNα, TH1 and myeloid responses in C57Bl/6 mice model[1].
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.

Animal Model: C57Bl/6 mice model[1]
Dosage: 1, 5, 10, and 50 mg/kg
Administration: p.o. once
Result: Induced IFNα at low dose as well as TH1 and myeloid responses at higher doses.
Animal Model: AAV-HBV C57Bl/6 mice model[1]
Dosage: 5 mg/kg
Administration: p.o., once a week, 8 weeks
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.
Animal Model: cynomolgus monkeys model[1]
Dosage: 3, 9, and 30 mg/kg
Administration: p.o., once
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.
Molecular Weight

254.33

Formula

C12H22N4O2
CAS No.
SMILES

NC(N=C1N[C@H](CCO)CCCC)=NC=C1OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TLR7/8 agonist 13 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TLR7/8 agonist 131402802-45-2Toll-like Receptor (TLR)HBVIFNARInterleukin RelatedHepatitis B virusInterferon-α/β receptorInterferon-alpha/beta receptor ILAgonisthPBMCcynomolgus monkeysAAV-HBV infectionhepatitis B virusInhibitorinhibitorinhibit

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