N-(4-acetamidophenyl)-Indomethacin amide

Potent and selective reversible inhibitor of COX-2

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1mg

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220.00

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5mg

￥1212.00

970.00

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10mg

￥2175.00

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50mg

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货号: ajci5464
CAS: 261766-23-8
别名: N-4AIA
分子式: C27H24ClN3O4
分子量: 490
纯度: >98%
溶解度: ≤16mg/ml in DMSO;16mg/ml in dimethyl formamide
储存: Store at -20°C
库存: 现货

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].

Reference:
[1].? Kalgutkar AS, Marnett AB, Crews BC, et al. Ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors. J Med Chem. 2000 Jul 27;43(15):2860-70.