Tolmetin是一种具有口服活性的，有效的COX抑制剂，对人COX-1和COX-2的IC50值分别为0.35µM和0.82µM。Tolmetin属于非甾体类物质，具有强效的抗炎活性。
货号:ajcx31582
CAS:26171-23-3
分子式:C15H15NO3
分子量：257.28
溶解度:DMSO: 100 mg/mL (388.68 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Tolmetin is an orally active and potent COX inhibitor with IC50s of 0.35 µM and 0.82 µM human COX-1 and COX-2, respectively. Tolmetin is a non-steroidal anti-inflammatory drug (NSAID)[1][2].

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[3].Tolmetin (0.001-100 μM) shows anticancer activity againts HT-29 colon cancer cell line in a dose-dependent manner[4].Tolmetin (0-100 μM) shows no effect on osteoblast growth[5].

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[2]. Tolmetin (5 mg/kg twice a day for 5 days) pre-treatment considerably attenuates quinolinic acid (QA)-induced neurotoxicity[3].

[1]. T D Warner, et al. Nonsteroid drug selectivities for cyclo-oxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: a full in vitro analysis. Proc Natl Acad Sci U S A. 1999 Jun 22;96(13):7563-8. [2]. DADA?, Yakup, et al. Synthesis and anticancer activity of some novel tolmetin thiosemicarbazides. Marmara Pharmaceutical Journal 19(3) • April 2015 [3]. Etcheverry SB, et al. Three new vanadyl(IV) complexes with non-steroidal anti-inflammatory drugs (Ibuprofen, Naproxen and Tolmetin). Bioactivity on osteoblast-like cells in culture. J Inorg Biochem. 2002 Jan 1;88(1):94-100. [4]. Etcheverry SB, et al. Three new vanadyl(IV) complexes with non-steroidal anti-inflammatory drugs (Ibuprofen, Naproxen and Tolmetin). Bioactivity on osteoblast-like cells in culture. J Inorg Biochem. 2002 Jan 1;88(1):94-100. [5]. Etcheverry SB, et al. Three new vanadyl(IV) complexes with non-steroidal anti-inflammatory drugs (Ibuprofen, Naproxen and Tolmetin). Bioactivity on osteoblast-like cells in culture. J Inorg Biochem. 2002 Jan 1;88(1):94-100.