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CAS No.: 181695-72-7

Valdecoxib/伐地考昔 Catalog No. CSN12344

Synonyms: SC 65872;Bextra;伐地考昔

Valdecoxib is a potent COX inhbitor that selectively inhibitors COX-2 with IC50 of 5 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 COX2

IC50:5nM
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 ... more >> Postoperative Pain Collapse <<	Phase 4	Unknown	June 2012	China, Guangdong ... more >> 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 Collapse <<
NCT03092193	Poor Metabolizer Due to Cytoch... more >>rome P450 CYP2C9 Variant Poor Metabolizer Due to Cytochrome p450 CYP2C19 Variant Collapse <<	Phase 4	Recruiting	December 2018	Brazil ... more >> Bauru School of Dentistry/USP Recruiting Bauru, São Paulo, Brazil, 17012-901 Contact: Adriana M Calvo, PhD 551432358276 birinjela@yahoo.com.br Collapse <<

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.1811 mL
- 15.9054 mL
- 31.8108 mL
- 5 mM
- 0.6362 mL
- 3.1811 mL
- 6.3622 mL
- 10 mM
- 0.3181 mL
- 1.5905 mL
- 3.1811 mL

技术信息

CAS号

181695-72-7

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H14N2O3S

运输

蓝冰

分子量

314.36

别名

SC 65872;Bextra;伐地考昔;帕瑞考昔钠

溶解度

DMSO	63.0 mg/mL (200.4 mM)
Water	Insoluble
Ethanol	16.0 mg/mL (50.9 mM)

动物实验配方

0.5% methylcellulose+0.2% Tween 80+water

19 mg/mL

suspension

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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 ... more >> Postoperative Pain Collapse <<	Phase 4	Unknown	June 2012	China, Guangdong ... more >> 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 Collapse <<
NCT03092193	Poor Metabolizer Due to Cytoch... more >>rome P450 CYP2C9 Variant Poor Metabolizer Due to Cytochrome p450 CYP2C19 Variant Collapse <<	Phase 4	Recruiting	December 2018	Brazil ... more >> Bauru School of Dentistry/USP Recruiting Bauru, São Paulo, Brazil, 17012-901 Contact: Adriana M Calvo, PhD 551432358276 birinjela@yahoo.com.br Collapse <<
NCT00602901	Subacute Low Back Pain ... more >> Chronic Low Back Pain Collapse <<	Phase 2	Completed	-	United States, Iowa ... more >> Palmer Center for Chiropractic Research Davenport, Iowa, United States, 52803 The University of Iowa Iowa City, Iowa, United States, 52242 Collapse <<
NCT00115752	Pain	Phase 2	Completed	-	United States, Maryland ... more >> National Institute of Nursing Research (NINR) Bethesda, Maryland, United States, 20892 Collapse <<
NCT01361789	Rupture of Anterior Cruciate L... more >>igament Collapse <<	Phase 4	Completed	-	Norway ... more >> Baerum Hospital Rud, Norway, 1309 Collapse <<
NCT00285649	Low Back Pain	Not Applicable	Completed	-	United States, Iowa ... more >> Palmer Center for Chiropractic Research Davenport, Iowa, United States, 52803 Collapse <<
NCT01541137	Postoperative Pain	Not Applicable	Completed	-	Finland ... more >> Helsinki University Central Hospital Helsinki, Finland Collapse <<
NCT00763997	Platelet Aggregation	Not Applicable	Completed	-	Germany ... more >> BG University Hospital Bergmannsheil GmbH Bochum, Germany, 44789 Collapse <<
NCT00092339	Postoperative Pain	Phase 3	Completed	-	-
NCT00092300	Postoperative Pain	Phase 3	Completed	-	-
NCT00122096	Neurosurgery ... more >>Pain Collapse <<	Phase 4	Completed	-	United States, Washington ... more >> University of Washington Seattle, Washington, United States, 98195 Collapse <<
NCT00636064	Pain	Phase 3	Completed	-	-
NCT00650624	Osteoarthritis, Knee	Phase 2	Completed	-	Japan ... more >> Pfizer Investigational Site Funabashi, Chiba, Japan Pfizer Investigational Site Sakura, Chiba, Japan Pfizer Investigational Site Chikushi-gun, Fukuoka, Japan Pfizer Investigational Site Iizuka, Fukuoka, Japan Pfizer Investigational Site Kurume, Fukuoka, Japan Pfizer Investigational Site Yame, Fukuoka, Japan Pfizer Investigational Site Chitose, Hokkaido, Japan Pfizer Investigational Site Sapporo, Hokkaido, Japan Pfizer Investigational Site Kamakura, Kanagawa, Japan Pfizer Investigational Site Yokohama, Kanagawa, Japan Pfizer Investigational Site Isahaya, Nagasaki, Japan Pfizer Investigational Site Hirakata, Osaka, Japan Pfizer Investigational Site Kanzaki-gun, Saga, Japan Pfizer Investigational Site Karatsu, Saga, Japan Pfizer Investigational Site Ogi-gun, Saga, Japan Pfizer Investigational Site Itabashi-ku, Tokyo, Japan Pfizer Investigational Site Setagaya-ku, Tokyo, Japan Pfizer Investigational Site Shinjuku-Ku, Tokyo, Japan Pfizer Investigational Site Taito-ku, Tokyo, Japan Pfizer Investigational Site Yoyogi Shibuya-ku, Tokyo, Japan Pfizer Investigational Site Saga, Japan Pfizer Investigational Site Tokyo, Japan Collapse <<
NCT00650039	Pain	Phase 3	Completed	-	-
NCT00649415	Dysmenorrhea	Phase 4	Completed	-	Brazil ... more >> Pfizer Investigational Site Salvador, Bahia, Brazil Pfizer Investigational Site Goiania, Goias, Brazil Pfizer Investigational Site Belo Horizonte, Minas Gerais, Brazil, 30130-100 Pfizer Investigational Site Belo Horizonte, Minas Gerais, Brazil, 30130-110 Pfizer Investigational Site Porto Alegre, Rio Grande Do Sul, Brazil, 90610-000 Pfizer Investigational Site Rio De Janeiro, RJ, Brazil, 20551-030 Pfizer Investigational Site Porto Alegre, RS, Brazil Pfizer Investigational Site São Paulo, SP, Brazil Pfizer Investigational Site Sao Paulo, Brazil Pfizer Investigational Site São Paulo, Brazil, 04062-003 Collapse <<
NCT00650598	Pain, Postoperative	Phase 4	Completed	-	Australia, South Australia ... more >> Pfizer Investigational Site Adelaide, South Australia, Australia, SA 5000 Hong Kong Pfizer Investigational Site Hong Kong, Hong Kong Pfizer Investigational Site Shatin, New Territories, Hong Kong Korea, Republic of Pfizer Investigational Site Seoul, Korea, Republic of, 110-744 Pfizer Investigational Site Seoul, Korea, Republic of, 138-736 Pfizer Investigational Site Seoul, Korea, Republic of, 140-757 Pfizer Investigational Site Seoul, Korea, Republic of Malaysia Pfizer Investigational Site Cheras, Kuala Lumpur, Malaysia, 56000 Pfizer Investigational Site Kuala Lumpur, Wilayah Persekutuan, Malaysia, 50586 Pfizer Investigational Site Kuala Lumpur, Wilayah Persekutuan, Malaysia, 59100 New Zealand Pfizer Investigational Site Auckland, New Zealand Pfizer Investigational Site Christchurch, New Zealand Pfizer Investigational Site Wellington, New Zealand Philippines Pfizer Investigational Site Manila, Philippines Pfizer Investigational Site Quezon City, Philippines Pfizer Investigational Site Quezon, Philippines Singapore Pfizer Investigational Site Singapore, Singapore, 529889 Taiwan Pfizer Investigational Site Kaohsiung, Taiwan Pfizer Investigational Site Keelung, Taiwan Pfizer Investigational Site Taipei, Taiwan Thailand Pfizer Investigational Site Bangkok, Thailand, 10330 Pfizer Investigational Site Bangkok, Thailand, 10400 Pfizer Investigational Site Bangkok, Thailand, 10700 Pfizer Investigational Site Bangkok, Thailand Collapse <<
NCT00647829	Pharyngitis	Phase 3	Completed	-	United States, Connecticut ... more >> Pfizer Investigational Site Storrs, Connecticut, United States, 06269-2011 United States, Florida Pfizer Investigational Site Boca Raton, Florida, United States, 33433 Collapse <<
NCT00260325	Pain Hyperalg... more >>esia Collapse <<	Phase 4	Completed	-	United States, Pennsylvania ... more >> Penn State University College of Medicine Hershey, Pennsylvania, United States, 17033 Collapse <<
NCT00653354	Pain, Post-surgical	Phase 3	Completed	-	United States, Arizona ... more >> Pfizer Investigational Site Phoenix, Arizona, United States, 85015 Pfizer Investigational Site Phoenix, Arizona, United States, 85016 Pfizer Investigational Site Phoenix, Arizona, United States, 85020 Pfizer Investigational Site Phoenix, Arizona, United States, 85032 Pfizer Investigational Site Tempe, Arizona, United States, 85281 United States, California Pfizer Investigational Site Anaheim, California, United States, 92701 Pfizer Investigational Site Chula Vista, California, United States, 91911 Pfizer Investigational Site San Diego, California, United States, 92114 Pfizer Investigational Site Santa Ana, California, United States, 92701 Pfizer Investigational Site Tustin, California, United States, 92780 United States, Kentucky Pfizer Investigational Site Lexington, Kentucky, United States, 40504 Pfizer Investigational Site Lexington, Kentucky, United States, 40509 Pfizer Investigational Site Lexington, Kentucky, United States, 40515 United States, Pennsylvania Pfizer Investigational Site Altoona, Pennsylvania, United States, 16602 Pfizer Investigational Site Duncansville, Pennsylvania, United States, 16635 United States, Tennessee Pfizer Investigational Site Johnson City, Tennessee, United States, 37601 Pfizer Investigational Site Johnson City, Tennessee, United States, 37604 United States, Texas Pfizer Investigational Site San Antonio, Texas, United States, 78229 Pfizer Investigational Site San Antonio, Texas, United States, 78240 United States, Utah Pfizer Investigational Site Salt Lake City, Utah, United States, 84117 Pfizer Investigational Site Salt Lake City, Utah, United States, 84123 Collapse <<
NCT00648258	Osteoarthritis	Phase 3	Completed	-	Taiwan ... more >> Pfizer Investigational Site Kweishan, Taoyuan, Taiwan Pfizer Investigational Site Kaohsiung, Taiwan Pfizer Investigational Site Taichung, Taiwan Pfizer Investigational Site Taipei, Taiwan Collapse <<
NCT00021996	Pain Unspecif... more >>ied Adult Solid Tumor, Protocol Specific Collapse <<	Not Applicable	Completed	-	United States, Massachusetts ... more >> Brigham and Women's Hospital Boston, Massachusetts, United States, 02115 Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 Collapse <<
NCT00651300	Pain	Phase 3	Terminated(See Detailed Descri... more >>ption field.) Collapse <<	-	Australia, New South Wales ... more >> Pfizer Investigational Site Port Macquarie, New South Wales, Australia Pfizer Investigational Site Randwick, New South Wales, Australia, 2031 Pfizer Investigational Site Westmead, New South Wales, Australia, 2145 Australia, Queensland Pfizer Investigational Site Coopers Plain, Queensland, Australia, 4108 Pfizer Investigational Site Townsville, Queensland, Australia, 4814 Australia, Victoria Pfizer Investigational Site Heidelberg, Victoria, Australia, 3084 Pfizer Investigational Site Prahran, Victoria, Australia, 3181 Australia, Western Australia Pfizer Investigational Site Perth, Western Australia, Australia, 6847 Collapse <<
NCT00661635	Laparoscopic Cholecystectomy ... more >> Pain Collapse <<	Phase 3	Completed	-	-
NCT00652808	Osteoarthritis ... more >> Knee Collapse <<	Phase 3	Completed	-	Korea, Republic of ... more >> Pfizer Investigational Site Anyang, Korea, Republic of, 431-070 Pfizer Investigational Site Gwangju, Korea, Republic of, 501-757 Pfizer Investigational Site Incheon, Korea, Republic of, 405-760 Pfizer Investigational Site Pusan, Korea, Republic of, 602-739 Pfizer Investigational Site Seoul, Korea, Republic of, 110-744 Pfizer Investigational Site Seoul, Korea, Republic of, 137-701 Pfizer Investigational Site Seoul, Korea, Republic of, 138-736 Pfizer Investigational Site Seoul, Korea, Republic of, 152-703 Collapse <<
NCT00671320	Pain Sprains ... more >>and Strains Sprain Collapse <<	Phase 4	Completed	-	Argentina ... more >> Pfizer Investigational Site Avellaneda, Buenos Aires, Argentina, 1872 Pfizer Investigational Site San Isidro, Buenos Aires, Argentina, 1642 Pfizer Investigational Site Buenos Aires, Argentina Chile Pfizer Investigational Site Santiago, RM, Chile Pfizer Investigational Site Santiago, Chile Colombia Pfizer Investigational Site Medellin, Antioquia, Colombia, (574) 5141516 Pfizer Investigational Site Bogota, Cundinamarca, Colombia, (57) 310-2322198 Pfizer Investigational Site Bogota, Cundinamarca, Colombia, (57) 310-8849622 Pfizer Investigational Site Bogota, Cundinarmarca, Colombia, (571) 6 164278 Pfizer Investigational Site Bucaramanga, Santander, Colombia, (577) 6 395409 Pfizer Investigational Site Cali, Valle del Cauca, Colombia, (57) 315-5410469 Pfizer Investigational Site Calli, Valle del Cauca, Colombia, (57) 310-8259712 Mexico Pfizer Investigational Site Monterrey, Nuevo Leon, Mexico, 64460 Peru Pfizer Investigational Site Lima, Peru, 27 Pfizer Investigational Site Lima, Peru Collapse <<
NCT00657449	Acute Pain	Phase 4	Terminated(See termination rea... more >>son in detailed description.) Collapse <<	-	Brazil ... more >> Instituto Ortopedico de Goiania Goiania, Goias, Brazil, 74210-030 Centro de Traumatologia e Ortopedia Goiania, Goiás, Brazil Hospital Mãe de Deus Porto Alegre, RIO Grande DO SUL, Brazil, 90880480 Hospital Sao Zacarias Rio de Janeiro, RJ, Brazil Grupo Hospitalar Conceiçao Porto Alegre, RS, Brazil, 91350200 Hospital Geral do Grajau São Paulo, SP, Brazil, 04822-320 Unifesp - Hsp São Paulo, Brazil, 04063003 SECONCI São Paulo, Brazil, 05001000 Collapse <<
NCT00683137	Pain Hallux V... more >>algus Collapse <<	Phase 3	Completed	-	-
NCT00649610	Low Back Pain	Phase 4	Completed	-	Argentina ... more >> Pfizer Investigational Site Bs. As., Argentina Pfizer Investigational Site Buenos Aires, Argentina, C1221ACI Brazil Pfizer Investigational Site Goiania, Goias, Brazil, 74085-450 Pfizer Investigational Site Curitiba, Parana, Brazil, 80430-210 Pfizer Investigational Site Curitiba, PR, Brazil Pfizer Investigational Site Petropolis, Rio de Janeiro, Brazil, 25620-040 Pfizer Investigational Site Sao Paulo, SP, Brazil, 04023-900 Pfizer Investigational Site Sao Paulo, SP, Brazil, 04029-000 Pfizer Investigational Site Sao Paulo, SP, Brazil, 05403-012 Pfizer Investigational Site Sao Paulo, Brazil, 05001-000 Chile Pfizer Investigational Site Santiago, Chile Colombia Pfizer Investigational Site Bogota, D.c., Colombia Pfizer Investigational Site Bogota D.c, Colombia Pfizer Investigational Site Cali-valle, Colombia Costa Rica Pfizer Investigational Site Cartago City, Cartago, Costa Rica, 7051 Pfizer Investigational Site Hatillo, San Jose, Costa Rica, 476-1002 Ecuador Pfizer Investigational Site Quito, Pichincha, Ecuador Mexico Pfizer Investigational Site Toluca, Edo. de Mexico, Mexico, 50080 Pfizer Investigational Site Zapopan, Jalisco, Mexico, 45040 Pfizer Investigational Site Zapopan, Jalisco, Mexico, 45200 Pfizer Investigational Site Puebla, Mexico, 72000 Pfizer Investigational Site Puebla, Mexico, 72070 Pfizer Investigational Site Puebla, Mexico, 72410 Peru Pfizer Investigational Site Lima, Peru, LIMA 11 Pfizer Investigational Site Lima, Peru, LIMA 27 Venezuela Pfizer Investigational Site Caracas, DF, Venezuela, 1020 Pfizer Investigational Site Caracas, DF, Venezuela, 1051 Pfizer Investigational Site Caracas, DF, Venezuela, 1070 Pfizer Investigational Site Caracas, Venezuela Collapse <<
NCT00419549	ERCP Pancreat... more >>itis Collapse <<	Phase 2 Phase 3	Terminated(Because one of the ... more >>drugs Valdecoxib was withdrawn due to safety concerns.) Collapse <<	-	India ... more >> All India Institute of Medical Sciences New Delhi, India Collapse <<
NCT00660855	Pain, Post Surgical	Phase 4	Terminated(See Detailed Descri... more >>ption.) Collapse <<	-	Argentina ... more >> Pfizer Investigational Site Buenos Aires, Argentina, C1230AAW Pfizer Investigational Site Buenos Aires, Argentina, C1280AEB Collapse <<
NCT00650455	Arthritis, Rheumatoid	Phase 4	Completed	-	-

Valdecoxib/伐地考昔 Catalog No. CSN12344

靶点选择性

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