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Etodolac

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Chemical Structure| 41340-25-4 同义名 : AY-24236;NIH 9918;NSC 282126;(±)-Etodolac
CAS号 : 41340-25-4
货号 : A128494
分子式 : C17H21NO3
纯度 : 99%
分子量 : 287.353
MDL号 : MFCD00133313
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(365.4 mM)，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 4 mg/mL clear

PO 0.5% CMC-Na 32 mg/mL suspension

生物活性
靶点

  • COX
描述 Etodolac, a selective cyclooxygenase-2 (COX-2) inhibitor, is a non-steroidal anti-inflammatory drug. Etodolac contributes to protection against rejection after heart transplantation. Etodolac could therefore be used to suppress graft rejection by means of its anti-inflammatory properties[3]. Etodolac is a nonsteroidal antiinflammatory drug (NSAID) that is available by prescription only and is used long term for therapy of chronic arthritis and short term for acute pain[4]. The decrease in the paw-withdrawal threshold induced by paclitaxel was reversed by oral administration of etodolac at 10 mg/kg but was not affected by indomethacin, diclofenac, or celecoxib. The antiallodynic effect of etodolac gradually increased during repeated administration, and after 2 weeks the paw-withdrawal threshold at the preadministration point was significantly increased. Etodolac probably acts at the level of functional changes accompanying paclitaxel treatment, such as alterations in the activation state of components of the pain transmission pathway[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
NCT01506154 Bursitis Tend... 展开 >>onitis Shoulder Pain 收起 << Phase 3 Completed - -
NCT00527319 Cachexia Phase 2 Completed - United States, Texas ... 展开 >> First Dynamic Health Care Services, Inc. Waco, Texas, United States, 76708 India Rajalakshmi Nursing Home Bangalore, India Nizam Institute of Medical Sciences Hyderabaad, India Orchid Nursing Home Kolkata, India Shatabdi Super Specialty Hospital Nashik, India All India Institute of Medical Sciences New Delhi, India Indraprastha Apollo Hospital New Delhi, India Deenanath Mangeshkar Hospital Pune, India 收起 <<
NCT01638962 Osteoarthritis, Knee Not Applicable Completed - Denmark ... 展开 >> University of Southern Denmark Odense, Region Syddanmark, Denmark, 5230 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.48mL

0.70mL

0.35mL

17.40mL

3.48mL

1.74mL

34.80mL

6.96mL

3.48mL
参考文献

[1]Kumagai K, Kubo M, et al. The COX-2 selective blocker etodolac inhibits TNFα-induced apoptosis in isolated rabbit articular chondrocytes. Int J Mol Sci. 2013 Sep 30;14(10):19705-15.

[2]Ito S, Tajima K, et al. Etodolac, a cyclooxygenase-2 inhibitor, attenuates paclitaxel-induced peripheral neuropathy in a mouse model of mechanical allodynia. J Pharmacol Exp Ther. 2012 Jul;342(1):53-60.

[3]Matsuyama M, Yoshimura R, Hase T, Chargui J, Yoshimura N, Touraine JL. Administration of the selective cyclooxygenase (COX)-2 inhibitor etodolac prolongs cardiac allograft survival in a mouse model. Mol Med Rep. 2010;3(5):771-774

[4]Etodolac. In: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; April 5, 2018

[5]Ito S, Tajima K, Nogawa M, et al. Etodolac, a cyclooxygenase-2 inhibitor, attenuates paclitaxel-induced peripheral neuropathy in a mouse model of mechanical allodynia. J Pharmacol Exp Ther. 2012;342(1):53-60