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Indomethacin N-octyl amide Sale

目录号 : GC14777

Indomethacin with enhanced selectivity for COX-2

Indomethacin N-octyl amide Chemical Structure

Cas No.:282728-65-8

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1mg
¥333.00
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5mg
¥1,491.00
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10mg
¥2,617.00
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50mg
¥11,405.00
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Sample solution is provided at 25 µL, 10mM.

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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.

Chemical Properties

Cas No. 282728-65-8 SDF
化学名 N-octyl-1-(4-chlorobenzoyl)-5-methoxy-1H-indole-3-acetamide
Canonical SMILES ClC1=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°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.1322 mL 10.661 mL 21.322 mL
5 mM 0.4264 mL 2.1322 mL 4.2644 mL
10 mM 0.2132 mL 1.0661 mL 2.1322 mL
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