Anti-inflammatory agent 130
Anti-inflammatory agent 130 is an anti-inflammatory agent. Anti-inflammatory agent 130 selectively induces and stabilizes the p65 G4 structure (Kd = 12.9 μM), thereby inhibiting p65 transcription, reducing p65 protein expression and its translocation to the nucleus, and ultimately inhibiting the NF-κB signaling pathway. Anti-inflammatory agent 130 attenuates acute lung injury and ameliorates ulcerative colitis in mice.
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- Formule: C34H40N6O4S3
- Masse moléculaire:692.91
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Description
In Vitro
Anti-inflammatory agent 130 (0.0195-20 μM) binds p65 G4 with a KD of 12.9 μM, and its binding to dsDNA or ssDNA is undetectable[1].
Anti-inflammatory agent 130 (10 μM) induces G4 formation in RAW264.7 cells, increasing BG4 foci to more than 13 per cell[1].
Anti-inflammatory agent 130 increases BG4 enrichment at the p65 promoter in RAW264.7 cells to 10.8%[1].
Anti-inflammatory agent 130 (2.5-10.0 μM; 24 h) shows low cytotoxicity in RAW264.7 cells, with a survival rate of 79.34% at 10 μM[1].
Anti-inflammatory agent 130 (2.5-10.0 μM) inhibits p65 mRNA in RAW264.7 cells[1].
Anti-inflammatory agent 130 (2.5-10.0 μM) reduces the accumulation of total p65 and nuclear p65 in LPS-stimulated RAW264.7 cells[1].
Anti-inflammatory agent 130 (2.5-10.0 μM) inhibits the nuclear translocation of p65 in LPS-stimulated RAW264.7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW264.7 macrophages
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Concentration:10 μM
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Incubation Time:overnight at 4 °C (BG4 antibody); 1.5 h (secondary antibody)
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Result:Control cells had 0 BG4 foci per cell.
At 10 μM, increased BG4 foci to more than 13 per cell, and LPS stimulation further enhanced G4 formation.
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Cell Line:RAW264.7 macrophages
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Concentration:2.5, 5.0, 10.0 μM
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Incubation Time:24 h (C38); 4 h (MTT)
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Result:Maintained cell viability above 80% up to 10 μM with or without LPS.
In Table 4, cell viability at 10 μM was 79.34%.
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Cell Line:RAW264.7 macrophages
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Concentration:2.5, 5.0, 10.0 μM
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Incubation Time:overnight at 4 °C (p65 antibody); 1.5 h (secondary antibody)
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Result:Dose-dependently suppressed LPS-induced nuclear translocation of p65.
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Cell Line:RAW264.7 macrophages
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Concentration:10 μM
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Incubation Time:30 min (C38 pre-incubation); 24 h (LPS stimulation)
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Result:At 10 μM, inhibited IL-6 by 92.44% and TNF-α by 84.10%.
Also dose-dependently suppressed LPS-induced IL-6 and IL-1β expression and secretion at 2.5, 5.0, and 10.0 μM.
In Vivo
Anti-inflammatory agent 130 (5-20 mg/kg; i.p.; daily) dose-dependently ameliorates DSS-induced ulcerative colitis in mice, reducing disease activity, colon shortening, colonic injury and fibrosis, inflammatory cell infiltration, and local and systemic proinflammatory cytokine levels[1].
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, 18-22 g, 6-8 weeks old)[1]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:i.p.; at 24 h, 12 h, and 1 h before LPS challenge
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Result:Dose-dependently ameliorated LPS-induced inflammatory cell infiltration, alveolar structural disruption, and interstitial edema.
At 20 mg/kg, lung architecture was nearly normal.
Dose-dependently reduced lung injury scores and lung wet/dry weight ratio, decreased BALF total protein concentration and total cell counts, and reduced F4/80-positive macrophage and LY-6G-positive neutrophil infiltration in lung tissue.
Dose-dependently reduced IL-6, TNF-α, and IL-1β levels in BALF, suppressed their mRNA expression in lung tissue, and lowered circulating cytokine levels.
Reduced total p65 and phosphorylated p65 protein levels in lung tissue and inhibited p65 nuclear translocation.
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Animal Model:C57BL/6 (male, 18-22 g, 6-8 weeks old)[1]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:i.p.; daily
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Result:Reduced body weight loss, decreased disease activity index, and improved colon shortening.
Attenuated DSS-induced colonic epithelial disruption, crypt damage, and inflammatory infiltration and dose-dependently restored intestinal architecture.
Reduced collagen deposition and fibrosis, increased PAS-positive mucus production, and upregulated MUC2 expression in a dose-dependent manner.
Reduced F4/80-positive macrophage and LY-6G-positive neutrophil infiltration in colonic tissue.
Downregulated TNF-α and IL-6 in colonic tissue, intestinal mucus, and serum in a dose-dependent manner.
Inhibited p65 nuclear translocation and reduced total p65 and phosphorylated p65 levels in colonic tissue.
Chemical Information
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Masse moléculaire 692.91
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Formule C34H40N6O4S3
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SMILES
O=C(NC1=CC2=C(C=C1)C(NC3=CC(S(=O)(C)=O)=CC=C3)=C4C(C=C(C=C4)NC(CCN5CCSCC5)=O)=N2)CCN6CCSCC6
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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)
Anti-inflammatory agent 130 Related Classifications
HY-190747 Related Classifications
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