AF-45
AF-45 inhibits IRAK4 and IRAK1, with IC50s of 128 nM and 1765 nM. AF-45 inhibits the release of IL-6 and TNF-α in macrophages, with IC50s of 0.53-1.54 μM and 0.6-2.75 μM. AF-45 is also an inhibitor for NF-κB/MAPK signaling pathway. AF-45 exhibits anti-inflammatory activities against DSS-induced ulcerative colitis and Lipopolysaccharide (HY-D1056)-induced acute lung injury in mouse model. AF-45 exhibits good pharmacokinetic characteristics in rat models.
For research use only. We do not sell to patients.
- Formula: C22H25N3O3
- Molecular Weight:379.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
IRAK4 128 nM (IC50) |
IRAK1 1765 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| J774.A1 | IC50 |
1.54 μM
Compound: d5; AF-45
|
Antiinflammatory activity in LPS-induced mouse J774.A1 cells assessed as inhibition of IL-6 release pretreated for 30 mins followed by LPS stimulation and measured after 24 hrs by ELISA
Antiinflammatory activity in LPS-induced mouse J774.A1 cells assessed as inhibition of IL-6 release pretreated for 30 mins followed by LPS stimulation and measured after 24 hrs by ELISA
|
[PMID: 38913701] |
| J774.A1 | IC50 |
2.75 μM
Compound: d5; AF-45
|
Antiinflammatory activity in LPS-induced mouse J774.A1 cells assessed as inhibition of TNF-alpha release pretreated for 30 mins followed by LPS stimulation and measured after 24 hrs by ELISA
Antiinflammatory activity in LPS-induced mouse J774.A1 cells assessed as inhibition of TNF-alpha release pretreated for 30 mins followed by LPS stimulation and measured after 24 hrs by ELISA
|
[PMID: 38913701] |
| RAW264.7 | IC50 |
1.27 μM
Compound: d5; AF-45
|
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of IL-6 release pretreated for 30 mins followed by LPS stimulation and measured after 24 hrs by ELISA
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of IL-6 release pretreated for 30 mins followed by LPS stimulation and measured after 24 hrs by ELISA
|
[PMID: 38913701] |
| RAW264.7 | IC50 |
2.6 μM
Compound: d5; AF-45
|
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of TNF-alpha release pretreated for 30 mins followed by LPS stimulation and measured after 24 hrs by ELISA
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of TNF-alpha release pretreated for 30 mins followed by LPS stimulation and measured after 24 hrs by ELISA
|
[PMID: 38913701] |
| THP-1 | IC50 |
0.53 μM
Compound: d5; AF-45
|
Antiinflammatory activity in LPS-induced human THP-1 cells assessed as inhibition of IL-6 release pretreated for 30 mins followed by LPS stimulation and measured after 24 hrs by ELISA
Antiinflammatory activity in LPS-induced human THP-1 cells assessed as inhibition of IL-6 release pretreated for 30 mins followed by LPS stimulation and measured after 24 hrs by ELISA
|
[PMID: 38913701] |
| THP-1 | IC50 |
0.6 μM
Compound: d5; AF-45
|
Antiinflammatory activity in LPS-induced human THP-1 cells assessed as inhibition of TNF-alpha release pretreated for 30 mins followed by LPS stimulation and measured after 24 hrs by ELISA
Antiinflammatory activity in LPS-induced human THP-1 cells assessed as inhibition of TNF-alpha release pretreated for 30 mins followed by LPS stimulation and measured after 24 hrs by ELISA
|
[PMID: 38913701] |
Chemical Information
-
Molecular Weight 379.45
-
Formula C22H25N3O3
-
SMILES
COC1=CC2=C(N=CN=C2O[C@H]3CC[C@@H](N)CC3)C=C1OCC4=CC=CC=C4
-
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)