Aceclofenac

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Chemical Structure| 89796-99-6 同义名 : Preservex; Airtal; Beofenac; YT-919
CAS号 : 89796-99-6
货号 : A683045
分子式 : C16H13Cl2NO4
纯度 : 98%
分子量 : 354.18
MDL号 : MFCD00864296
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 Aceclofenac is a non-steroidal anti-inflammatory drug (NSAID) analog of Diclofenac. Aceclofenac has higher anti-inflammatory action than conventional NSAIDs. It is a cytokine inhibitor. Aceclofenac works by blocking the action of a substance in the body called cyclo-oxygenase. Aceclofenac inhibited COX-2 more potently than COX-1 (IC50: 3.0/7.3 microM)[3]. Oral administration of aceclofenac induced significant gastric ulceration, which was inhibited by esomeprazole administration. Co-administration of esomeprazole with aceclofenac may reduce aceclofenac-induced gastrointestinal complications without significant pharmacokinetic interactions[4]. In patients with CLBP (chronic lower back pain), aceclofenac CR(controlled release) and aceclofenac demonstrated significant symptomatic pain relief, improvement in quality of life and functional scores[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
NCT01912066 NSAID-associated Gastroduodena... 展开 >>l Injury 收起 << Phase 4 Completed - Korea, Republic of ... 展开 >> Inje University Busan Paik Hospital Busan, Korea, Republic of, 614735 收起 <<
NCT01952314 Ureter Stones Phase 3 Completed - Korea, Republic of ... 展开 >> Donguk University Ilsan Hospital Goyang, Kyunggi, Korea, Republic of Seoul National University Bundang Hospital Seongnam, Kyunggi, Korea, Republic of, 463-712 Kangwon National University Hospital Chuncheon, Korea, Republic of Seoul National University Hospital Seoul, Korea, Republic of, 110-744 National Medical Center Seoul, Korea, Republic of Seoul National University Boramae Medical Center Seoul, Korea, Republic of 收起 <<
NCT02384928 Sciatica Inte... 展开 >>rvertebral Disc Displacement 收起 << Not Applicable Completed - Korea, Republic of ... 展开 >> Jaseng Hospital of Korean Medicine Seoul, Gangnam-Gu, Korea, Republic of, 135-896 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.82mL

0.56mL

0.28mL

14.12mL

2.82mL

1.41mL

28.23mL

5.65mL

2.82mL
参考文献

[1]Narayan R, Pednekar A, et al. A top-down technique to improve the solubility and bioavailability of aceclofenac: in vitro and in vivo studies. Int J Nanomedicine. 2017 Jul 11;12:4921-4935.

[2]Jana S, Sen KK. Chitosan - Locust bean gum interpenetrating polymeric network nanocomposites for delivery of aceclofenac. Int J Biol Macromol. 2017 Sep;102:878-884.

[3]Dannhardt G, Ulbrich H. In-vitro test system for the evaluation of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) inhibitors based on a single HPLC run with UV detection using bovine aortic coronary endothelial cells (BAECs). Inflamm Res. 2001;50(5):262-269

[4]Kim TH, Thapa SK, Lee DY, et al. Pharmacokinetics and Anti-Gastric Ulceration Activity of Oral Administration of Aceclofenac and Esomeprazole in Rats. Pharmaceutics. 2018;10(3):152. Published 2018 Sep 6

[5]Yang JH, Suk KS, Lee BH, et al. Efficacy and Safety of Different Aceclofenac Treatments for Chronic Lower Back Pain: Prospective, Randomized, Single Center, Open-Label Clinical Trials. Yonsei Med J. 2017;58(3):637-643