产品说明书

Valdecoxib

Print
Chemical Structure| 181695-72-7 同义名 : 代他考昔 ;SC 65872
CAS号 : 181695-72-7
货号 : A727456
分子式 : C16H14N2O3S
纯度 : 99+%
分子量 : 314.359
MDL号 : MFCD00950568
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(111.34 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：

0.5% methylcellulose+0.2% Tween 80+water 19 mg/mL suspension

生物活性
靶点

  • COX-2

    COX-2, IC50:5 nM
描述 Valdecoxib is a highly potent and selective inhibitor of COX-2, with IC50s of 5 nM and 140 μM for COX-2 and COX-1, respeceively[3]. Valdecoxib inhibited LPS-induced proliferation of endothelial cells and bFGF secretion in a dose-dependent manner. Valdecoxib stimulated VEGF formation via HMEC-1 (human microvascular endothelial cells) under inflammatory conditions[4]. Valdecoxib (10 mg/kg, i.p.) significantly attenuates the behavioral and biochemical (oxidative damage) alterations in chronic-stressed mice[5]. Valdecoxib has the symptomatic treatment of osteoarthritis or rheumatoid arthritis (10 to 20 mg once a day) and for the treatment of primary dysmenorrhea (40 mg once a day). Valdecoxib is as efficacious as conventional non-COX-2 selective NSAIDs, but offers the advantage of a much better gastrointestinal tolerance[6]. In acute post-surgical pain, valdecoxib provided similar pain relief to oxycodone/paracetamol, had a long duration of action, a rapid onset of analgesia and was opioid-sparing[7].
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
NCT00285649 - Completed - -
NCT01221025 Emergence Delirium ... 展开 >> Postoperative Pain 收起 << Phase 4 Unknown June 2012 China, Guangdong ... 展开 >> The First Affiliated Hospital of Sun Yat-sen University Recruiting Guangzhou, Guangdong, China, 510080 Contact: Haihua Shu, MD; Ph D    +86-20-87755766 ext 8273    shuhaihua@gmail.com 收起 <<
NCT03092193 Poor Metabolizer Due to Cytoch... 展开 >>rome P450 CYP2C9 Variant Poor Metabolizer Due to Cytochrome p450 CYP2C19 Variant 收起 << Phase 4 Recruiting December 2018 Brazil ... 展开 >> Bauru School of Dentistry/USP Recruiting Bauru, São Paulo, Brazil, 17012-901 Contact: Adriana M Calvo, PhD    551432358276    birinjela@yahoo.com.br 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.18mL

0.64mL

0.32mL

15.91mL

3.18mL

1.59mL

31.81mL

6.36mL

3.18mL
参考文献

[1]Gierse JK, Zhang Y, et al. Valdecoxib: assessment of cyclooxygenase-2 potency and selectivity. J Pharmacol Exp Ther. 2005 Mar;312(3):1206-12.

[2]Talley JJ, Brown DL, et al. 4-[5-Methyl-3-phenylisoxazol-4-yl] - benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2. J Med Chem. 2000 Mar 9;43(5):775-7.

[3]Talley JJ, Brown DL, Carter JS, Graneto MJ, Koboldt CM, Masferrer JL, Perkins WE, Rogers RS, Shaffer AF, Zhang YY, Zweifel BS, Seibert K. 4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2. J Med Chem. 2000 Mar 9;43(5):775-7

[4]Wiktorowska-Owczarek A. The effect of valdecoxib on the production of growth factors evoked by hypoxia and bacterial lipopolysaccharide in HMEC-1 cells. Adv Clin Exp Med. 2013 Nov-Dec;22(6):795-800

[5]Kumar A, Kumari B, Kumar P. Protective effects of selective and non-selective cyclooxygenase inhibitors in an animal model of chronic stress. Neurosci Bull. 2010 Feb;26(1):17-27

[6]Scheen AJ, Malaise M. Le médicament du mois. Valdécoxib (Bextra) [Valdecoxib (Bextra)]. Rev Med Liege. 2004 Apr;59(4):251-4. French

[7]Fenton C, Keating GM, Wagstaff AJ. Valdecoxib: a review of its use in the management of osteoarthritis, rheumatoid arthritis, dysmenorrhoea and acute pain. Drugs. 2004;64(11):1231-61