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CAS No.: 53164-05-9

Acemetacin/阿西美辛 Catalog No. CSN10202

Synonyms: TVX 1322;K-708;Rantudil

Acemetacin is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor.

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技术信息

生物活性

描述Acemetacin is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor. With purified COX-1(cyclo-oxygenase), inhibition was absent with nimesulide, weak with acemetacin (inhibitory concentration of 50% [IC50 ] 85 m̈mol/L), and potent with indomethacin (IC50 0.6 m̈mol/L). Acemetacin did not inhibit sheep COX-2 and only weakly inhibited COX-1^[3]. Acemetacin is a prodrug of indomethacin that exhibits better gastric tolerability in preclinical and clinical trials. Equimolar doses of acemetacin or indomethacin were administered orally. The antihyperalgesic and antiinflammatory effects were also similar for both indomethacin and acemetacin^[4]. The increased gastric and intestinal tolerability of acemetacin may be related to the lack of induction of leukocyte-endothelial adherence. This may be attributable to the reduced ability of acemetacin to elevate leukotriene-B(4) synthesis and TNF-alpha expression, compared to indomethacin, despite the fact that acemetacin is rapidly bioconverted to indomethacin after its absorption^[5].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01759355	-	-	Active, not recruiting	May 2019	United States, North Carolina ... more >> University of North Carolina-Chapel Hill Chapel Hill, North Carolina, United States, 27599 Collapse <<

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4049 mL
- 12.0243 mL
- 24.0487 mL
- 5 mM
- 0.4810 mL
- 2.4049 mL
- 4.8097 mL
- 10 mM
- 0.2405 mL
- 1.2024 mL
- 2.4049 mL

技术信息

CAS号

53164-05-9

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H18ClNO6

运输

蓝冰

分子量

415.82

别名

TVX 1322;K-708;Rantudil;阿西美辛

溶解度

DMSO	82.0 mg/mL (197.2 mM)
Water	Insoluble
Ethanol	58.0 mg/mL (139.5 mM) warming

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