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N-(2-phenylethyl)-Indomethacin amide

 
Catalog No.
C5628
COX-2抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 1,408.00
Ship with 10-15 days
10mg
¥ 2,491.00
Ship with 10-15 days
50mg
¥ 8,233.00
Ship with 10-15 days

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A

背景

N-(2-phenylethyl)-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-(2-phenylethyl)-Indomethacin amide (N-2PIA) is a reversible, potent and selective COX-2 inhibitor that inhibits human recombinant COX-2 and ovine COX-1 with IC50 values of 0.06 and >66 μM, respectively. It is over 1000 times less potent as an inhibitor of ovine COX-1. N-(2-phenylethyl)-Indomethacin amide is an analogous derivative of indomethacin that shows selective against COX-2 [1].

In the carageenan-induced foot pad edema assay, orally administration of N-2PIA 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.

化学属性

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt461
Cas No.261766-32-9
FormulaC27H25ClN2O3
SynonymsN-2PIA
Solubility≤80mg/ml in ethanol;10mg/ml in DMSO;14mg/ml in dimethyl formamide
Chemical NameN-(2-phenylethyl)-1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetamide
SDFDownload SDF
Canonical SMILESO=C(CC1=C(C)N(C(C2=CC=C(Cl)C=C2)=O)C3=C1C=C(OC)C=C3)N([H])CCC4=CC=CC=C4
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化学结构

N-(2-phenylethyl)-Indomethacin amide