您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Nabumetone
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Nabumetone
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。
Nabumetone图片
CAS NO:42924-53-8
包装与价格:
包装价格(元)
500 mg电议
1 g电议
1 mL*10 mM(in DMSO)电议

产品名称
BRL14777
萘丁美酮
产品介绍
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。

产品描述

Nabumetone(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.

Cas No.

42924-53-8

分子式

C15H16O2

分子量

228.291

别名

BRL14777;萘丁美酮

储存和溶解度

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