Tolmetin (Synonyms: 托麦汀)
目录号: PL05553 纯度: ≥98%
CAS No. :26171-23-3
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中文名称
Tolmetin
中文别名
托麦汀;2-[1-甲基-5-(4-甲基苯甲酰)吡咯-2-基]乙酸;托美汀
英文名称
Tolmetin
英文别名
1-Methyl-5-p-toluoylpyrrole-2-acetic acid;2-[1-Methyl-5-(4-methylbenzoyl)-pyrrol-2-yl]acetic acid;2-[1-methyl-5-(4-methylbenzoyl)pyrrol-2-yl]acetic acid;TOLMETIN;[3H]-Tolmetin;1-methyl-5-(4-methylbenzoyl)-1H-pyrrole-2-acetic acid;1-methyl-5-(4-methylbenzoyl)pyrrol-2-acetic acid;2-(1-Methyl-5-(4-methylbenzoyl)-1H-pyrrol-2-yl)acetic acid;5-(4-methylbenzoyl)-1-methyl-pyrrol-2-ylace;5-(p-toluoyl)-1-methylpyrrole-2-acetic acid;Tolectin;Tolmetina;Tolmetina [DCIT];Tolmetine [INN-French];Tolmetino;Tolmetinum;Tolmetine;Tolmetinum [INN-Latin];Tolmetino [INN-Spanish];1H-Pyrrole-2-acetic acid, 1-methyl-5-(4-methylbenzoyl)-;MCN 2559;1-Methyl-5-(4-methylbenzoyl)-pyrrole-2-acetic acid;Acido 1-metil-5-(p-tolnil)-pirrol-2-acetico;EIN
Cas No.
26171-23-3
分子式
C15H15NO3
分子量
257.28
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
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 0.35 µM 和 0.82 µM。Tolmetin 属于非甾体类物质,具有强效的抗炎活性。
生物活性
Tolmetin is an orally active and potent COX inhibitor with IC 50 s of 0.35 μM and 0.82 μM human COX-1 and COX-2, respectively. Tolmetin is a non-steroidal anti-inflammatory drug (NSAID).
性状
Solid
IC50 & Target[1][2]
Human COX-1 0.35 μM (IC50) Human COX-2 0.8
体外研究(In Vitro)
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.
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[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
溶解度数据
In Vitro: DMSO : 100 mg/mL (388.68 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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