N-(4-acetamidophenyl)-Indomethacin amide

- Overview
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    Background
    
    N-(4-acetamidophenyl)-Indomethacin amide is a reversible, potent and selective COX-2 inhibitor [1]. Cyclooxygenase (COX) is an enzyme responsible for formation of prostanoids, including thromboxane and prostaglandins such as prostacyclin. COX-1 is the constitutive isoform and is mainly responsible for the synthesis of cytoprotective prostaglandins in the gastrointestinal tract (GI) and of the proaggregatory thromboxane in blood platelets. COX-2 is inducible and short-lived that is stimulated by endotoxin, cytokines, and mitogens. COX-2 plays important roles in prostaglandin biosynthesis in inflammatory cells the central nervous system [1]. N-(4-acetamidophenyl)-indomethacin amide (N-4-AIA) is a reversible, potent and selective COX-2 inhibitor that inhibits human recombinant COX-2 and ovine COX-1 with IC50 values of 0.12 and >66 μM, respectively. It is over 550 times less potent as an inhibitor of ovine COX-1. N-(4-acetamidophenyl)-indomethacin amide is the 4-acetamidophenyl derivative of indomethacin that shows selective against COX-2 [1]. In the carageenan-induced foot pad edema assay, orally administration of N-4-AIA showed anti-inflammatory activity [1].
- Properties
  - Alternative Name
    
    N-4AIA; N-(4-acetamidophenyl)-1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetamide
    
    CAS Number
    
    261766-23-8
    
    Molecular Formula
    
    C27H24ClN3O4
    
    Molecular Weight
    
    490
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤16mg/ml in DMSO;16mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

N-(4-acetamidophenyl)-Indomethacin amide

N-(4-acetamidophenyl)-Indomethacin amide

Background

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