Anti-inflammatory agent 122
Anti-inflammatory agent 122 is an orally active anti-inflammatory agent. Anti-inflammatory agent 122 inhibits the activation of the NF-κB signaling cascade. Anti-inflammatory agent 122 downregulates the phosphorylation levels of JNK, p38 MAPK and ERK, thereby inhibiting the activation of the MAPK pathway. Anti-inflammatory agent 122 reduces the levels of pro-inflammatory cytokines TNF-α, IL-1β, iNOS and COX-2. Anti-inflammatory agent 122 alleviates paw swelling symptoms in rats with adjuvant-induced arthritis. Anti-inflammatory agent 122 can be used in studies related to adjuvant-induced arthritis.
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- Formel: C24H18N4O3
- Molecular Weight:410.42
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Speicherung:
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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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
IL-1β |
iNOS |
COX-2 |
In Vitro
Anti-inflammatory agent 122 (Compound d12) (10-20 μM; 24 h) exhibits no obvious cytotoxicity against RAW264.7 macrophages at concentrations of 10 μM and 20 μM, with cell viability maintained at >80% under both concentrations[1].
Anti-inflammatory agent 122 (2.5-10 μM; 1 h) dose-dependently downregulates LPS-induced iNOS and COX-2 expression, and inhibits the activation of JNK/p38/ERK MAPK pathway and p65/IκB NF-κB pathway in RAW264.7 macrophages[1].
Anti-inflammatory agent 122 (0.6125-20 μM; 1 h) potently inhibits LPS-induced NO production in RAW264.7 macrophages, with an IC50 of 3.96 μM and an inhibition rate of 88.04% at a concentration of 10 μM[1].
Anti-inflammatory agent 122 modulates gene expression in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages, and exerts anti-inflammatory effects primarily by inhibiting the MAPK and TNF signaling pathways[1].
Anti-inflammatory agent 122 (1.25-20 μM; 1 h) dose-dependently inhibits LPS-induced TNF-α and IL-1β secretion in RAW264.7 macrophages, with IC50 values of 5.31 μM and 7.14 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:murine macrophage RAW264.7 cells
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Concentration:10 μM; 20 μM
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Incubation Time:24 h
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Result:Maintained RAW264.7 cell viability >80% at 10 μM.
Maintained RAW264.7 cell viability >80% at 20 μM, causing no apparent cytotoxicity.
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Cell Line:LPS-stimulated murine macrophage RAW264.7 cells
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Concentration:1.25 μM; 2.5 μM; 5 μM; 10 μM; 20 μM
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Incubation Time:1 h pretreatment, followed by 24 h LPS stimulation
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Result:Dose-dependently decreased LPS-induced TNF-α levels, with an IC50 value of 5.31 μM.
Dose-dependently decreased LPS-induced IL-1β levels, with an IC50 value of 7.14 μM.
Showed superior efficacy to indomethacin at 10 μM.
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Cell Line:LPS-stimulated murine macrophage RAW264.7 cells
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Concentration:2.5 μM; 5 μM; 10 μM
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Incubation Time:1 h pretreatment, followed by 24 h LPS stimulation
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Result:Dose-dependently reduced the phosphorylation levels of JNK, p38, ERK, p65, and IκB.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (SD) (female, adjuvant-induced arthritis model)[1]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:p.o.; daily; 14 days
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Result:Reduced right hind paw thickness compared to the AIA model group.
Decreased arthritis index scores compared to the AIA model group.
Gradually restored body weight compared to the AIA model group.
Alleviated synovial hyperplasia, inflammatory cell infiltration, and cartilage erosion in ankle joints compared to the AIA model group.
Reduced serum TNF-α levels to ~750 pg/mL (30 mg/kg) and ~900 pg/mL (10 mg/kg), compared to ~1350 pg/mL in the model group.
Reduced serum IL-1β levels to ~75 pg/mL (30 mg/kg) and ~120 pg/mL (10 mg/kg), compared to ~135 pg/mL in the model group.
Exhibited a therapeutic effect comparable to indomethacin at 30 mg/kg.
Chemical Information
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Molecular Weight 410.42
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Formel C24H18N4O3
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SMILES
O=C(NC1=CC(C2=O)=C(N3C2=NC4=C(C=CC=C4)C3=O)C=C1)C(N)CC5=CC=CC=C5
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Anti-inflammatory agent 122 Related Classifications
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