Anti-inflammatory agent 113
Anti-inflammatory agent 113 (compound B5) is a Cathepsin L (CTSL) inhibitor and anti-inflammatory agent with a CTSL IC50 of 5.52 μM. Anti-inflammatory agent 113 suppresses CTSL maturation, attenuates NF-κB and p38 MAPK signaling pathway activation, and binds stably in CTSL’s active site via noncovalent interactions with Asp162, Cys25, and Glu63. Anti-inflammatory agent 113 inhibits pro-inflammatory cytokine (IL-6, IL-8) production, reduces inflammatory cell lung infiltration, and alleviates lung tissue injury. Anti-inflammatory agent 113 can be used for the research of acute lung injury.
For research use only. We do not sell to patients.
- Formula: C27H24N6O
- Molecular Weight:448.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Anti-inflammatory agent 113 (compound B5) (0.30-10 μM; 30 min pretreatment, 24 h LPS incubation) potently and dose-dependently inhibits LPS-induced IL-6 (IC50=2.51 μM) and IL-8 (IC50=1.15 μM) production in HBE cells[1].
Anti-inflammatory agent 113 (0.30-10 μM; 30 min pretreatment, 24 h LPS incubation) potently and dose-dependently inhibits LPS-induced IL-6 (IC50=0.76 μM) and IL-8 (IC50=4.06 μM) production in THP-1 cells[1].
Anti-inflammatory agent 113 (0.30-10 μM; 30 min pretreatment, 24 h LPS incubation) potently and dose-dependently inhibits LPS-induced IL-6 production in Raw 264.7 cells with an IC50 of 0.73 μM[1].
Anti-inflammatory agent 113 (0.625-5 μM; 30 min pretreatment, 16 h LPS stimulation) concentration-dependently inhibits LPS-induced CTSL maturation in HBE cells[1].
Anti-inflammatory agent 113 (0.625-5 μM; 30 min pretreatment, 16 h LPS stimulation) concentration-dependently inhibits LPS-induced activation of the NF-κB and p38 MAPK signaling pathways in HBE cells[1].
Anti-inflammatory agent 113 (0.001-100 μM; 30 min) potently inhibits CTSL enzymatic activity with an IC50 of 5.52 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human bronchial epithelial (HBE) cells
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Concentration:0.30-10 μM
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Incubation Time:30 min (pretreatment); 24 h (LPS incubation)
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Result:Exhibited dose-dependent inhibition of IL-6 and IL-8 production, with IC50 values of 2.51 μM for IL-6 and 1.15 μM for IL-8.
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Cell Line:Raw 264.7 cells
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Concentration:0.30-10 μM
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Incubation Time:30 min (pretreatment); 24 h (LPS incubation)
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Result:Inhibited IL-6 production with an IC50 value of 0.73 μM.
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Cell Line:HBE cells
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Concentration:0.625-5 μM
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Incubation Time:30 min (pretreatment); 16 h (LPS stimulation)
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Result:Inhibited LPS-induced CTSL maturation in a clear, concentration-dependent manner.\nReduced LPS-induced levels of phospho-IκBα, phospho-p65, and phospho-p38, indicating suppression of NF-κB and p38 MAPK pathway activation.
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, 20-25 g)[1]
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Dosage:10 mg/kg; 20 mg/kg
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Administration:i.p.; daily; 3 days
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Result:Significantly reduced inflammatory cell infiltration in lung tissue and preserved alveolar architecture compared to the LPS-only group at 10 mg/kg and 20 mg/kg.
Significantly suppressed LPS-induced increases in IL-6 and TNF-α levels in bronchoalveolar lavage fluid (BALF), reduced total cell counts and total protein concentrations in BALF, and decreased the lung wet-to-dry weight ratio at 20 mg/kg.
Downregulated LPS-induced CTSL expression in mouse lung tissue.
Chemical Information
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Molecular Weight 448.52
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Formula C27H24N6O
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SMILES
O=C(NC1=CC=CC(NC2=NC=CC(C3=CNC4=C3C=CC=C4)=N2)=C1)[C@@H](N)CC5=CC=CC=C5
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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)
Anti-inflammatory agent 113 Related Classifications
HY-181676 Related Classifications
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