TLR7/8 agonist 14
TLR7/8 agonist 14 is a TLR7 and TLR8 agonist with EC50 values of 0.53 μM and 4.3 μM, respectively. TLR7/8 agonist 14 increases the secretion of the proinflammatory cytokines TNF-α, IL-1β, IL-8 and IFN-γ. TLR7/8 agonist 14 increases cytokine secretion and expression of CD86. LR7/8 agonist 14 can be used for research colorectal carcinoma.
For research use only. We do not sell to patients.
- Formula: C17H23ClN2O2
- Molecular Weight:322.83
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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TLR7 0.53 μM (EC50) |
TLR8 4.3 μM (EC50) |
IL-1β |
IL-8 |
TNF-α |
TLR7/8 agonist 14 (compound 69) (1-5 μM, 24 h) exhibits immunomodulatory properties in PBMCs[1].
TLR7/8 agonist 14 (5 μM, 24 h) increases the expression of the co-stimulatory molecule CD86[1].
TLR7/8 agonist 14 (20 μM) activates the downstream MyD88-dependent signaling pathway, leading to AP-1 activation and inducing phosphorylation of MEK-1, p38, IκB, and ERK1/2 in THP-1 cells, thereby activating downstream signaling pathways[1].
TLR7/8 agonist 14 (10 mM, 1 h) has t1/2 (min) = 5.6, CLint (mic)(μL/min/mg) = 246.9, CLint (liver)(ml/min/kg) = 222.2 in human liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human peripheral blood mononuclear cells (PBMCs)
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Concentration:1 μM; 5 μM
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Incubation Time:24 h
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Result:Increased the secretion of the inflammatory cytokines TNF-α, IL-1β, and IL-8.
Increase IL-6 slightly.
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Cell Line:Immature dendritic cells
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Concentration:5 μM
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Incubation Time:24 h
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Result:Increased CD86 expression.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CT26 murine colorectal carcinoma cells (0.3 × 106 in 100 μL of sterile 0.9 % NaCl, s.c.) induced female BALB/c mice (8-10 weeks, 19-21 g)[1]
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Dosage:2.5, 5, or 10 mg/kg
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Administration:s.c., 2.5 mg/kg single injection, 5 mg/kg single injection, 10 mg/kg single injection, 2.5 mg/kg triple injections, 5 mg/kg triple injections, 10 mg/kg triple injections.
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Result:Had a dose-and frequency-dependent inhibition of tumor growth.
Suppressed tumor growth and increased survival time (10 mg/kg triple injections).
Resulted in a modest delay in tumor growth (approximately 3 days).
Resulted in a robust and statistically significant suppression of tumor growth.
Resulted in 8 days of tumor growth delay.
Resulted a 2.7-fold increase at the highest dose tested.
Resulted also in significantly increased survival of mice.
Chemical Information
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Molecular Weight 322.83
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Formula C17H23ClN2O2
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SMILES
O=C1N(C(CCCCCC)CO)C=NC2=C1C(C)=CC=C2Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TLR7/8 agonist 14 Related Classifications
HY-179336 Related Classifications
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