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Acemetacin

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Chemical Structure| 53164-05-9 同义名 : TVX 1322
CAS号 : 53164-05-9
货号 : A374323
分子式 : C21H18ClNO6
纯度 : 98%
分子量 : 415.824
MDL号 : MFCD00151473
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(288.58 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • COX
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 ... 展开 >> University of North Carolina-Chapel Hill Chapel Hill, North Carolina, United States, 27599 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.40mL

0.48mL

0.24mL

12.02mL

2.40mL

1.20mL

24.05mL

4.81mL

2.40mL
参考文献

[1]Chavez-Pina AE, McKnight W, et al. Mechanisms underlying the anti-inflammatory activity and gastric safety of acemetacin. Br J Pharmacol. 2007 Nov;152(6):930-8.

[2]Tavares IA, Bennett A. Acemetacin and indomethacin: differential inhibition of constitutive and inducible cyclo-oxygenases in human gastric mucosa and leucocytes. Int J Tissue React. 1993;15(2):49-53.

[3]Tavares IA, Bennett A. Non-steroidal anti-inflammatory drugs that cause relatively little gastric damage. J Gastroenterol Hepatol. 1998;13(S3):S190-S192

[4]Gil-Flores M, Ortiz MI, Castañeda-Hernández G, Chávez-Piña AE. Acemetacin antinociceptive mechanism is not related to NO or K+ channel pathways. Methods Find Exp Clin Pharmacol. 2010;32(2):101-105

[5]Chávez-Piña AE, Vong L, McKnight W, et al. Lack of effects of acemetacin on signalling pathways for leukocyte adherence may explain its gastrointestinal safety. Br J Pharmacol. 2008;155(6):857-864