2. Immunology/Inflammation Apoptosis
  3. Toll-like Receptor (TLR) Interleukin Related IFNAR TNF Receptor
  4. 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.

TLR7/8 agonist 14

TLR7/8 agonist 14 Chemical Structure

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TLR7/8 agonist 14 Related Antibodies

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Description

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[1].

IC50 & Target[1]

TLR7

0.53 μM (EC50)

TLR8

4.3 μM (EC50)

IL-1β

 

IL-8

 

TNF-α

 

In Vitro

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.

TLR7/8 agonist 14 Related Antibodies

ELISA Assay[1]

Cell Line: Human peripheral blood mononuclear cells (PBMCs)
Concentration: 1 μM; 5 μM
Incubation Time: 24 h
Result: Increased the secretion of the inflammatory cytokines TNF-α, IL-1β, and IL-8.
Increase IL-6 slightly.

Immunofluorescence[1]

Cell Line: Immature dendritic cells
Concentration: 5 μM
Incubation Time: 24 h
Result: Increased CD86 expression.
In Vivo

TLR7/8 agonist 14 (compound 69) (2.5-10 mg/kg, s.c., once or triple intratumoral at Day 1 Day 2 and Day 4) has potential antitumor activity without systemic toxicity in syngeneic mouse model of colorectal carcinoma (CT26)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage: 2.5, 5, or 10 mg/kg
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.
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.
Molecular Weight

322.83

Formula

C17H23ClN2O2
SMILES

O=C1N(C(CCCCCC)CO)C=NC2=C1C(C)=CC=C2Cl
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 14 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 14Toll-like Receptor (TLR)Interleukin RelatedIFNARTNF ReceptorILInterferon-α/β receptorInterferon-alpha/beta receptor Tumor Necrosis Factor ReceptorTNFRviral infectionsautoimmune diseasescolorectal carcinomaTLR7TLR8Inhibitorinhibitorinhibit

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