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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。
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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
100 mg | ¥ 195 | 现货 | |
500 mg | ¥ 418 | 现货 | |
1 g | ¥ 713 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 460 | 现货 |
产品描述 | Nabumetone (BRL14777)(BRL14777) is a non-steroidal anti-inflammatory drug and its active metabolite 6MNA inhibits the enzymes cyclo-oxygenase I and II. |
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。 |
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. |
别名 | BRL14777, 萘丁美酮 |
分子量 | 228.29 |
分子式 | C15H16O2 |
CAS No. | 42924-53-8 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 55 mg/mL (240.92 mM) Ethanol: 24 mg/mL (105.1 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
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