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26171-23-3

中文名稱 托麥汀
英文名稱 Tolmetin
CAS 26171-23-3
分子式 C15H15NO3
MDL 編號 MFCD00599595
分子量 257.29
MOL 文件 26171-23-3.mol
更新日期 2024/12/18 15:16:48
26171-23-3 結(jié)構(gòu)式 26171-23-3 結(jié)構(gòu)式

基本信息

中文別名
甲苯酰吡咯乙酸
痛滅定
托麥汀
托美汀
2-[1-甲基-5-(4-甲基苯甲酰)吡咯-2-基]乙酸
英文別名
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
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

熔點(diǎn)156 °C
沸點(diǎn)400.53°C (rough estimate)
密度1.1391 (rough estimate)
折射率1.5200 (estimate)
儲存條件Sealed in dry,2-8°C
溶解度可溶于氯仿(少許)、甲醇(少許)
酸度系數(shù)(pKa)pKa 3.5(H2O t undefined I undefined) (Uncertain)
形態(tài)固體
顏色灰白色至淡黃色
水溶解性222 mg/L
NIST化學(xué)物質(zhì)信息Tolmetin(26171-23-3)

安全數(shù)據(jù)

常見問題列表

生物活性
Tolmetin (Tolectin) 是一種非類固醇的抗炎藥,屬于雜環(huán)乙酸衍生物類,具有止痛和退熱作用。
靶點(diǎn)

Human COX-1

0.35 μM (IC 50 )

Human COX-2

0.82 μM (IC 50 )

體外研究

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.

體內(nèi)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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