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N-(2-phenylethyl)-Indomethacin amide
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
N-(2-phenylethyl)-Indomethacin amide图片
CAS NO:261766-32-9
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议

产品介绍
inhibitor of COX-2
Cas No.261766-32-9
别名N-2PIA
化学名N-(2-phenylethyl)-1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetamide
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
分子式C27H25ClN2O3
分子量461
溶解度≤80mg/ml in ethanol;10mg/ml in DMSO;14mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.