产品说明书

Etoricoxib

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Chemical Structure| 202409-33-4 同义名 : MK-0663;L-791456;Etoricoxib, Arcoxia, L-791456, MK 0663, MK-0663;Nucoxia;Algix;Tauxib;MK-663;Arcoxia
CAS号 : 202409-33-4
货号 : A137375
分子式 : C18H15ClN2O2S
纯度 : 99%
分子量 : 358.842
MDL号 : MFCD06797512
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(292.61 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：

IP 2% DMSO+2% Tween80+40% PEG300+water 10 mg/mL clear

PO 0.5% CMC-Na 65 mg/mL suspension

生物活性
靶点

  • COX-2
描述 Etoricoxib is a novel orally active agent that selectively inhibits cyclooxygenase-2 (COX-2). Etoricoxib is a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM, 116 μM and 5 μM for COX-2, COX-1 in human whole blood and purified human COX-2, respectively. Etoricoxib shows inhibitory effect on PGE2 production by CHO (COX-2) cells (IC50, 79 nM), on purified human COX-2 with detergent (IC50, 4.1 μM), and on purified PGE2 production by U937 microsomes (low substrate; IC50, 12.1 μM). However, Etoricoxib has little activity against COX-1 with a Ki of 167 μM[3]. Etoricoxib in 50 and 100 mg/kg doses changed the levels of oxidant/antioxidant parameters such as MDA, MPO, tGSH, GSHRd, GST, SOD, NO, and 8-OH/Gua in favour of antioxidants. Furthermore, etoricoxib prevented increase of COX-2 gene expression and ALT and AST levels[4]. Etoricoxib 120 mg administered orally once daily has the same efficacy on acute gout as indometacin and diclofenac. Etoricoxib is tolerated better by patients than NSAIDs such as indometacin and diclofenac[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
NCT01638962 Osteoarthritis, Knee Not Applicable Completed - Denmark ... 展开 >> University of Southern Denmark Odense, Region Syddanmark, Denmark, 5230 收起 <<
NCT00092729 Dysmenorrhea Phase 3 Completed - -
NCT03117894 Breast Neoplasm Female ... 展开 >> Regional Anesthesia Anesthesia Regional Anesthesia Morbidity Anesthesia Morbidity 收起 << Not Applicable Unknown December 2018 Sweden ... 展开 >> Östersund Hospital Recruiting Östersund, Jämtland, Sweden, 83183 Contact: Hans Ahlberg, MD    +4663153000    hans.ahlberg@regionjh.se    Contact: Joakim Johansson, PhD    +46703976410    joakim.johansson@regionjh.se 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.79mL

0.56mL

0.28mL

13.93mL

2.79mL

1.39mL

27.87mL

5.57mL

2.79mL
参考文献

[1]Jayaraman R, Manisenthil KT, et al. Influence of etoricoxib on anticonvulsant activity of phenytoin and diazepam in experimental seizure models in mice. J Pharm Pharmacol. 2010 May;62(5):610-4.

[2]Schiffmann S, Sandner J, et al. The selective COX-2 inhibitor celecoxib modulates sphingolipid synthesis. J Lipid Res. 2009 Jan;50(1):32-40.

[3]Riendeau D, Percival MD, Brideau C, et al. Etoricoxib (MK-0663): preclinical profile and comparison with other agents that selectively inhibit cyclooxygenase-2. J Pharmacol Exp Ther. 2001;296(2):558-566

[4]Kunak CS, Kukula O, Mutlu E, et al. The Effect of Etoricoxib on Hepatic Ischemia-Reperfusion Injury in Rats. Oxid Med Cell Longev. 2015;2015:598162

[5]Zhang S, Zhang Y, Liu P, Zhang W, Ma JL, Wang J. Efficacy and safety of etoricoxib compared with NSAIDs in acute gout: a systematic review and a meta-analysis. Clin Rheumatol. 2016;35(1):151-158