萘丁美酮 T1258

Product Introduction
Bioactivity


英文名: Nabumetone

描述: Nabumetone (BRL14777) 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。

激酶实验: 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.

体外活性: 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.

体内活性: 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。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 55 mg/mL (240.92 mM)
Ethanol : 24 mg/mL (105.1 mM)


关键字: Cyclooxygenase | Inhibitor | COX | inhibit | BRL 14777 | BRL-14777 | Nabumetone

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途