Anti-inflammatory agent 125
Anti-inflammatory agent 125 is an anti-inflammatory agent. Anti-inflammatory agent 125 inhibits the phosphorylation of p65 and IκBα induced by LPS (HY-D1056) stimulation, slows IκBα degradation, and inhibits the phosphorylation of p38 and ERK1/2, thereby simultaneously intervening in the NF-κB and MAPK pathways and reducing the production of IL-6 and IL-8. Anti-inflammatory agent 125 alleviates lung inflammation and edema and attenuates inflammatory cell infiltration in mouse models. Anti-inflammatory agent 125 exhibits low cytotoxicity in cells in vitro, with a favorable safety profile. Anti-inflammatory agent 125 can be used for research on acute lung injury and inflammation-related studies.
For research use only. We do not sell to patients.
- CAS No.: 3118064-89-1
- Formula: C18H12F2N4O2S
- Molecular Weight:386.38
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
IL-6 |
IL-8 |
p65 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HBE, THP-1, and RAW 264.7 cells
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Concentration:10 μM (HBE cytotoxicity assessment); >100 μM (cytotoxic IC50 in HBE, THP-1, and RAW 264.7 cells)
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Incubation Time:4 h
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Result:Showed no significant cytotoxicity in HBE cells at 10 μM.
Exhibited a favorable safety profile with inhibitory IC50 values exceeding 100 μM across HBE, THP-1, and RAW 264.7 cells.
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Cell Line:HBE, THP-1, and RAW 264.7 cells
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Concentration:5 μM
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Incubation Time:30 min (pre-incubation); 24 h (LPS stimulation)
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Result:Inhibited IL-6 and IL-8 release by 50.3% and 57.2%, respectively, in LPS-stimulated HBE cells.
Inhibition rates for both IL-6 and IL-8 exceeded 50%.
Exhibited concentration-dependent suppression of IL-6 and IL-8 in all three cell lines.
IL-6 inhibition IC50 values were 5.34 μM in HBE cells, 4.58 μM in THP-1 cells, and 4.15 μM in RAW 264.7 cells.
IL-8 inhibition IC50 values were 9.89 μM in HBE cells and 3.76 μM in THP-1 cells.
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Cell Line:HBE
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Concentration:1.25, 2.5, 5 and 10 μM
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Incubation Time:24 h
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Result:In LPS-stimulated HBE cells, it inhibited the activation of NF-κB (p65, IκBα phosphorylation, and IκBα degradation) and MAPK (p38 and ERK1/2 phosphorylation) pathways in a concentration-dependent manner, demonstrating a dual anti-inflammatory mechanism.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male)[1]
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Dosage:10 mg/kg (with LPS); 20 mg/kg (with LPS); 20 mg/kg (alone without LPS)
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Administration:intraperitoneal; once daily for 3 days; additional dose on day 4 at 1 h before intratracheal LPS in LPS groups
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Result:In LPS-induced ALI mice, B19 at 10 and 20 mg/kg alleviated inflammatory cell infiltration and pulmonary edema in lung tissue.
B19 reduced the lung wet-to-dry weight ratio, total protein content, and total cell counts in BALF.
B19 decreased BALF concentrations of IL-6 and TNF-α.
Histopathological lung injury scores were progressively reduced in a dose-dependent manner.
- Kinase activity and phosphorylation assays
- Western Blot
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Research Protocol for Inflammation-related Diseases
- Protocol for Kinase activity and phosphorylation assays
- Inhalation Toxicity Study
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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CAS No. 3118064-89-1
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Molecular Weight 386.38
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Formula C18H12F2N4O2S
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SMILES
FC1=CC(F)=CC=C1S(NC(C=CC=C2)=C2C3=C4C(NC=C4)=NC=N3)(=O)=O
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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)