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26171-23-3

中文名称 托麦汀
英文名称 Tolmetin
CAS 26171-23-3
分子式 C15H15NO3
MDL 编号 MFCD00599595
分子量 257.29
MOL 文件 26171-23-3.mol
更新日期 2024/04/22 14:21:56
26171-23-3 结构式 26171-23-3 结构式

基本信息

中文别名
甲苯酰吡咯乙酸
痛灭定
托麦汀
托美汀
2-[1-甲基-5-(4-甲基苯甲酰)吡咯-2-基]乙酸
英文别名
Tolmetin
Tolmetine
TOLMETINUM
2-[1-Methyl-5-(4-methylbenzoyl)-pyrrol-2-yl]acetic acid
1H-Pyrrole-2-acetic acid, 1-methyl-5-(4-methylbenzoyl)-
1-Methyl-5-p-toluoylpyrrole-2-acetic acid
5-[(p-Tolyl)carbonyl]-1-methylpyrrole-2-acetic acid
McN 2559
1-Methyl-5-(4-methylbenzoyl)-1H-pyrrole-2-acetic acid
1-Methyl-5-(p-toluoyl)-1H-pyrrole-2-acetic acid
所属类别
生物化工:激动剂抑制剂

物理化学性质

熔点156 °C
沸点400.53°C (rough estimate)
密度1.1391 (rough estimate)
折射率1.5200 (estimate)
储存条件Sealed in dry,2-8°C
溶解度可溶于氯仿(少许)、甲醇(少许)
酸度系数(pKa)pKa 3.5(H2O t undefined I undefined) (Uncertain)
形态固体
颜色灰白色至淡黄色
水溶解性222 mg/L
NIST化学物质信息Tolmetin(26171-23-3)

常见问题列表

生物活性
Tolmetin (Tolectin) 是一种非类固醇的抗炎药,属于杂环乙酸衍生物类,具有止痛和退热作用。
靶点

Human COX-1

0.35 μM (IC 50 )

Human COX-2

0.82 μM (IC 50 )

体外研究

Tolmetin (0.25 mM) does not attenuate lipid peroxidation in rat brain homogenate. Tolmetin (0.25, 0.5, 0.75, 1 mM) shows radical scavenging properties but without superoxide anion generation in rat brain homogenat.
Tolmetin (0.001-100 μM) shows anticancer activity againts HT-29 colon cancer cell line in a dose-dependent manner.
Tolmetin (0-100 μM) shows no effect on osteoblast growth.

体内研究

Tolmetin (30,100 mg/kg; gavage; single dose or twice daily for 3 and 14 days) shows maximal ulcerogenic effect 4 h after the single dose, while potently decreases after 3 and 14 days of repeated administration in male Wistar rats weighing 180-200 g. Tolmetin causes gastric lesions in 100 mg/kg.
Tolmetin (5 mg/kg twice a day for 5 days) pre-treatment considerably attenuates quinolinic acid (QA)-induced neurotoxicity.

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