1. NF-κB Metabolic Enzyme/Protease Apoptosis Immunology/Inflammation PI3K/Akt/mTOR
  2. NF-κB Glutathione Peroxidase TNF Receptor Interleukin Related mTOR SOD
  3. Anti-inflammatory agent 107

Anti-inflammatory agent 107 is an orally active anti-inflammatory agent. Anti-inflammatory agent 107 inhibits and NF-κB with a superior binding affinity of -9.4578 kcal/mol. Anti-inflammatory agent 107 reduces levels of inflammatory biomarkers (TNF-α, IL-6, INF-γ, NF-κβ, C-reactive protein and Erythrocyte Sedimentation Rate) and enhances the endogenous antioxidant defense system by elevating SOD (Superoxide Dismutase), CAT (Catalase) and GSH (Glutathione) activities. Anti-inflammatory agent 107 not induces liver toxicity and demonstrates hepatoprotective effects. Anti-inflammatory agent 107 dose-dependently ameliorates leukocyte infiltration and tissue edema. Anti-inflammatory agent 107 can be used for anti-inflammatory research.

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Anti-inflammatory agent 107

Anti-inflammatory agent 107 Chemical Structure

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Description

Anti-inflammatory agent 107 is an orally active anti-inflammatory agent. Anti-inflammatory agent 107 inhibits and NF-κB with a superior binding affinity of -9.4578 kcal/mol. Anti-inflammatory agent 107 reduces levels of inflammatory biomarkers (TNF-α, IL-6, INF-γ, NF-κβ, C-reactive protein and Erythrocyte Sedimentation Rate) and enhances the endogenous antioxidant defense system by elevating SOD (Superoxide Dismutase), CAT (Catalase) and GSH (Glutathione) activities. Anti-inflammatory agent 107 not induces liver toxicity and demonstrates hepatoprotective effects. Anti-inflammatory agent 107 dose-dependently ameliorates leukocyte infiltration and tissue edema. Anti-inflammatory agent 107 can be used for anti-inflammatory research[1].

IC50 & Target[1]

NF-κB

 

IL-6

 

mTOR

 

In Vitro

Anti-inflammatory agent 107 (compound 4D) exerts a powerful anti-inflammatory by suppressing NF-κβ with a docking score of 9.4578 kcal/mol, the primary inflammatory protein signaling[1].
Anti-inflammatory agent 107 (50 μg/mL in 2 mL, 50 μg/mL in 0.02 mL) shows potent anti-inflammatory activity in both the human red blood cell membrane stabilization (anti-hemolytic) assay and the protein denaturation inhibition assay[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Anti-inflammatory agent 107 (compound 4D) (20-50 μg/kg, p.o., once daily for a week) reduce inflammatory biomarkers, enhances and restores the antioxidant defenses (GSH, CAT, SOD) and renal toxicity, and reduces leukocyte infiltration in κ-Carrageenan (HY-138962)-induced paw edema rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: κ-Carrageenan (0.1 mL of 1 % W/V, inject into the subplantar region of the right hind paw, once)-induced male (Sprague Dawley) rats (120-125 g, 6-8 weeks)[1].
Dosage: 20, 30 and 50 μg/kg
Administration: p.o., once daily for a week
Result: Showed gradually improvement at different doses.
Showed gradually improvement, gave very close results compare to aspirin at 30 μg/kg.
Reduced levels of inflammatory biomarkers (TNF-α, IL-6, INF-γ, NF-κβ, CRP and ESR) at he high-dose 50 μg/kg.
Showed excellent malondialdehyde (MDA) and nitric oxide (NO) improvement especially at 30 and 50 μg/kg.
Reduced GSH concentrations, returned CAT and SOD activities to nearly normal ranges.
Showed good regression in hepatic enzyme secretion, total bilirubin conjugation and excretion, and albumin biosynthesis.
Reversed the carrageenan-induced renal toxicity (characterized by increased urea and creatinine) and restored these parameters to near-normal ranges.
Produced dose-dependent improvements in histopathology, reducing leukocyte infiltration at lower doses and nearly eliminating edema while restoring normal skin architecture at the highest dose (50 μg/kg).
Molecular Weight

628.57

Formula

C29H20N6O9S

SMILES

CCOC(C1=C(OC2=C(C1C3=CC=CO3)C(C4=CC=CS4)=NN2C5=CC=C(C=C5[N+]([O-])=O)[N+]([O-])=O)NC(C6=CN=CC=C6)=O)=O

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Anti-inflammatory agent 107
Cat. No.:
HY-179502
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