Nabumetone,42924-53-8

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YZ剂描述：

产品名称：Nabumetone

产品别名：萘丁美酮

英文别名：BRL14777

靶点：COX

CAS：42924-53-8

纯度：>99%

外观：白色或类白色结晶性粉末

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Nabumetone 是一种可口服的非酸类KY剂，为有效的、选择性的 COX-2 YZ剂，同时是活性代谢物 6MNA 的前体物质。

溶解性：DMSO : 43 mg/mL (188.4 mM)
Ethanol : 24 mg/mL (105.1 mM)

体外研究：

Nabumetone is a nonsteroidal anti-inflammatory prodrug. Nabumetone itself is non-acidic and, following absorption, it undergoes extensive first-pass metabolism to form the main circulating active metabolite (6-MNA) which is a much more potent inhibitor of preferentially COX-2.

体内研究：Nabumetone displays acute anti-inflammatory activity in the carrageenan-induced oedema model in rats and the ultraviolet-induced erythema model in guinea-pigs. Its activity in these tests is greater than that of aspirin but less than that of naproxen and indomethacin. In the cotton pellet-induced granuloma model in the rat, Nabumetone is active and produces no signs of toxicity at doses much greater than the lowest effective dose, unlike aspirin, naproxen or indomethacin. Nabumetone is also active in the adjuvant-induced arthritis test in rats. In contrast to aspirin, indomethacin and naproxen, Nabumetone is well tolerated by the stomach of fasted rats at doses in excess of those with anti-inflammatory activity.

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