中文名称:

托麦汀

中文同义词:

托美汀(托美汀酸);甲苯酰吡咯乙酸;痛灭定;托麦汀;托美汀;托美汀(托麦汀);2-[1-甲基-5-(4-甲基苯甲酰)吡咯-2-基]乙酸;托美汀溶液,100PPM

英文名称:

Tolmetin

英文同义词:

2-[1-methyl-5-[(4-methylphenyl)-oxomethyl]-2-pyrrolyl]acetic acid;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;C07149;2-(1-Methyl-5-(4-Methylbenzoyl)-1H-pyrrol-2-yl)acetic acid

CAS号:

26171-23-3

分子式:

C15H15NO3

分子量:

257.28

EINECS号:

247-497-2

相关类别:

医药中间体;小分子抑制剂;其他兽药标准品;小分子抑制剂，天然产物;化工中间体;医药原料;API intermediates;API;Inhibitors

Mol文件:

26171-23-3.mol

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

酸度系数(pKa)

pKa 3.5(H2O t undefined I undefined) (Uncertain)

水溶解性 

222 mg/L

NIST化学物质信息

Tolmetin(26171-23-3)

EPA化学物质信息

1H-Pyrrole-2-acetic acid, 1-methyl-5-(4-methylbenzoyl)- (26171-23-3)

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 )

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.

毒害物质数据

26171-23-3(Hazardous Substances Data)