TLR9 antagonist 2
TLR9 antagonist 2 is a highly selective and water-soluble TLR9 antagonist with an IC50 of 13 nM against human TLR9. TLR9 antagonist 2 inhibits CpG-induced production of the pro-inflammatory cytokine IL-6. TLR9 antagonist 2 is applicable for research on systemic, TLR9-mediated uncontrolled inflammatory responses, such as sepsis.
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- CAS No.: 1351978-48-7
- Formule: C25H36N6O2
- Masse moléculaire:452.60
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
[1]|
IL-6 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>10 μM
Compound: 18
|
Antagonist activity at human TLR8 transfected in HEK293 cells after 6 hrs by NF-kappaB luciferase reporter assay
Antagonist activity at human TLR8 transfected in HEK293 cells after 6 hrs by NF-kappaB luciferase reporter assay
|
[PMID: 25408837] |
| HEK293 | IC50 |
>970 nM
Compound: 18
|
Antagonist activity at human TLR7 transfected in HEK293 cells assessed as hydrolysis of pNPP after 24 hrs by SEAP reporter assay
Antagonist activity at human TLR7 transfected in HEK293 cells assessed as hydrolysis of pNPP after 24 hrs by SEAP reporter assay
|
[PMID: 25408837] |
| HEK293 | IC50 |
13 nM
Compound: 18
|
Antagonist activity at human TLR9 transfected in HEK293 cells after 6 hrs by NF-kappaB luciferase reporter assay
Antagonist activity at human TLR9 transfected in HEK293 cells after 6 hrs by NF-kappaB luciferase reporter assay
|
[PMID: 25408837] |
| PBMC | IC50 |
244 nM
Compound: 18
|
Inhibition of CpG-induced IL-6 production in human PBMC after 24 hrs by ELISA
Inhibition of CpG-induced IL-6 production in human PBMC after 24 hrs by ELISA
|
[PMID: 25408837] |
| Splenocyte | IC50 |
74 nM
Compound: 18
|
Inhibition of CpG-induced IL-6 production in C57BL/6 mouse splenocytes after 24 hrs by ELISA
Inhibition of CpG-induced IL-6 production in C57BL/6 mouse splenocytes after 24 hrs by ELISA
|
[PMID: 25408837] |
In Vitro
TLR9 antagonist 2 (Compound 18) inhibits CpG-induced IL-6 production in mouse splenocytes (IC50: 74 nM) and human peripheral blood mononuclear cells (PBMCs) (IC50: 244 nM) in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1351978-48-7
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Masse moléculaire 452.60
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Formule C25H36N6O2
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SMILES
OCCN1CCN(C=2C=CC(=CC2)C3=NC=C4C(=N3)N(CC4)CCCN5CCOCC5)CC1
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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)