Nabumetone 是一种非甾体抗炎药，是选择性COX-2抑制剂，其活性代谢物 6MNA 可抑制环加氧酶 I 和 II。

Nabumetone(BRL14777) is a non-steroidal anti-inflammatory drug and its active metabolite 6MNA inhibits the enzymes cyclo-oxygenase I and II.

在角叉菜胶诱导的大鼠水肿模型和紫外线诱发的豚鼠红疹模型中,Nabumetone具有抗炎活性.在大鼠肉芽肿瘤模型中,Nabumetone在高于最小有效剂量高的浓度,不会产生毒性.在患有佐剂性关节炎的大鼠中,Nabumetone在超过抗炎活性剂量下,对于大鼠的胃有良好的耐受性.

Nabumetone经过广泛的首过代谢,形成主循环活性代谢物(6-MNA),能够抑制COX-2。

Cells are harvested, washed, and lysed in NP-40 lysis buffer (50 mM Tris-HCl [pH 7.5], 150 mM NaCl, 0.5% NP-40). Total cell protein is quantified using the Bradford assay and 1-mg/mL protein aliquots are made. Ten microliters of total cell protein is mixed with 290 μL of substrate solution (0.1 mg/mL dithiothreitol [DTT], 0.1 mg/mL albumin, and 1 mM alanine-β-naphthylamide). Fluorometric measurements (340 nm excitation, 400 nm emission) are made after 15 and 30 min. The slope of the line between the 15- and 30-min measurements is used to represent aminopeptidase activity. Total cell protein is preincubated with bestatin, amastatin, puromycin, EDTA, and/or ZnCl2 for 20 min before the fluorometric aminopeptidase assay.

42924-53-8

C15H16O2

228.291

BRL14777;萘丁美酮

Ethanol:24 mg/mL (105.1 mM)
DMSO:43 mg/mL (188.4 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years