TLR8 antagonist-2
TLR8 antagonist-2 (Compound 35) is a selective TLR8 antagonist with an IC50 of 0.032 μM against hTLR8. TLR8 antagonist-2 potently inhibits TLR8-dependent NF-κB activity in cells stimulated with TL8-506 (HY-20457). TLR8 antagonist-2 can be used in research related to inflammatory and immune diseases.
For research use only. We do not sell to patients.
- Formula: C25H30N4O2
- Molecular Weight:418.53
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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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hTLR8 0.032 μM (IC50) |
TLR8 antagonist-2 (10 μM) potently inhibits TLR8-dependent NF-κB activity in hTLR8-HEK293 reporter cells stimulated by TL8-506, with an IC50 of 0.032 μM[1].
TLR8 antagonist-2 (1 h) potently inhibits TL8-506-induced TNF secretion, with an IC50 value of 0.014 μM in THP-1 macrophages and 0.107 μM in PBMCs[1].
TLR8 antagonist-2 potently inhibits the cellular responses of THP-1 macrophages stimulated by TL8-506, with an IC50 of 0.0022 μM[1].
The half-life of TLR8 antagonist-2 in mouse liver microsomes is 73.6 min[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1 macrophages, human peripheral blood mononuclear cells (PBMCs)
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Concentration:0.014 μM (THP-1 TNF IC50); 0.107 μM (PBMC TNF IC50); 1 μM (IL-8 inhibition); up to 50 μM (cytotoxicity test)
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Incubation Time:1 h (preincubation); 4 h (agonist stimulation)
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Result:Demonstrated concentration-dependent inhibition of TNF secretion, with an IC50 of 0.014 μM in THP-1 macrophages and 0.107 μM in PBMCs.
Completely inhibited TL8-506-induced IL-8 secretion at 1 μM in both cell types.
Showed no cytotoxicity detected up to 50 μM via LDH assay.
Chemical Information
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Molecular Weight 418.53
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Formula C25H30N4O2
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SMILES
O=C(NC1CCN(C(C)C)CC1)C2=CC=C(COC3=C4C=CC=CC4=NC(C)=N3)C=C2
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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)
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