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Indomethacin N-octyl 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。
Indomethacin N-octyl amide图片
CAS NO:282728-65-8
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
Cas No.282728-65-8
化学名N-octyl-1-(4-chlorobenzoyl)-5-methoxy-1H-indole-3-acetamide
Canonical SMILESClC1=CC=C(C(N2C(C=CC(OC)=C3)=C3C(CC(N([H])CCCCCCCC)=O)=C2C)=O)C=C1
分子式C27H33ClN2O3
分子量469.0
溶解度≤2mg/ml in ethanol;27mg/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

Indomethacin N-octyl amide is a potent and non-selective inhibitor of both COX-1 and COX-2 [1].

Cyclooxygenase (COX) is the key enzyme required for the conversion of arachidonic acid to prostaglandins. Cyclooxygenase enzymes have been involved in diverse physiological situations and disease processes ranging from inflammation to cancer. Until now, two cyclooxygenase isoforms have been identified, COX-1 and COX-2. The COX-1 enzyme is produced constitutively (i.e., gastric mucosa) and COX-2 is inducible (i.e., sites of inflammation) [2].

Indomethacin is a potent but non-selective inhibitor of both COX-1 and COX-2. Indomethacin is a substituted indole acetic acid, wherein the carboxylate can be derivitized as an ester or amide. Conversion of indomethacin into ester and amide derivatives provides a facile strategy for generating highly selective COX-2 inhibitors. Indomethacin N-octyl amide inhibited the activity of ovine COX-1 and human recombinant COX-2 with the IC50 values of 66 μM and 40 nM, respectively. While the IC50 of indomethacin for the inhibition of COX-1 and COX-2 were 0.67 μM and 0.05 μM, respectively [1].

References:
[1] Kalgutkar A S, Marnett A B, Crews B C, et al.  Ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors[J]. Journal of medicinal chemistry, 2000, 43(15): 2860-2870.
[2] Dubois R N, Abramson S B, Crofford L, et al.  Cyclooxygenase in biology and disease[J]. The FASEB journal, 1998, 12(12): 1063-1073.