Celecoxib是环氧合酶-2(COX-2)选择性抑制剂,IC50为40 nM。
In vitro, celecoxib not only reduced the production of PGE2 but also inhibited the downstream effects of PGE2. Celecoxib blocked migration and invasion of A549 cells increased by PGE2 in the wound healing and transwell assays. Additionally, celecoxib reduced MMP9 mRNA expression which was increased by PGE2. Moreover, celecoxib enhanced E-cadherin mRNA expression which was inhibited by PGE2.
0.5% methylcellulose+0.2% Tween 80
0 -75 μM
≤200 mg/kg 口服处理
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Penning TD, et al. J Med Chem, 1997, 40(9), 1347-1365.
[2] Silverstein, F.E., et al.: J. Am. Med. Assoc., 284, 1247 (2000)
[3] Steinbach, G., et al.: N. Engl. J. Med., 342, 1946 (2000)
分子式 C17H14F3N3O2S |
分子量 381.37 |
CAS号 169590-42-5 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 76 mg/mL |
Water <1 mg/mL |
Ethanol 30 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02131012 | Inflammation | Drug: Intravitreal Celecoxib | Vanderbilt University|Pfizer|Vanderbilt University Medical Center | Phase 1 | 2015-06-01 | 2017-02-20 |
NCT01344200 | Pharmacokinetics of Celecoxib in Children | Drug: Celecoxib | Children's Hospital of Eastern Ontario | Phase 4 | 2016-10-01 | 2016-08-17 |
NCT01695226 | Breast Neoplasms|Breast Cancer | Drug: celecoxib|Drug: Placebo | Pierre Hupperets|Maastricht University Medical Center | Phase 2 | 2004-02-01 | 2012-09-25 |
NCT00212108 | Nasopharyngeal Carcinoma | Drug: celecoxib, gefitinib | National University Hospital, Singapore|National Healthcare Group, Singapore | Phase 1|Phase 2 | 2003-11-01 | 2012-03-29 |
NCT02413203 | Healthy | Drug: Celecoxib|Drug: Placebo | University of Pennsylvania|Eli Lilly and Company | 2015-03-01 | 2016-04-21 | |
NCT02429427 | Breast Cancer | Drug: Celecoxib|Other: Placebo | Imperial College London|Institute of Cancer Research, United Kingdom | Phase 3 | 2005-12-01 | 2016-08-15 |
NCT00583453 | Tonsillitis | Drug: Celecoxib|Drug: Placebo | University of Iowa|Pfizer | Phase 2 | 2007-07-01 | 2013-12-11 |
NCT00030407 | Lung Cancer | Drug: Celecoxib|Drug: Docetaxel | Barbara Ann Karmanos Cancer Institute|National Cancer Institute (NCI) | Phase 2 | 2001-10-01 | 2013-04-25 |
NCT02779166 | Hip Labral Tears | Drug: Celecoxib|Drug: placebo | Northwestern University | 2012-08-01 | 2016-05-19 | |
NCT03067194 | Osteoarthritis Hand | Drug: Celecoxib 100 MG|Drug: Celecoxib 200mg | Chong Kun Dang Pharmaceutical | Phase 4 | 2016-12-01 | 2017-02-24 |
NCT01503385 | Lung Cancer | Drug: Celecoxib | Chinese Academy of Medical Sciences | Phase 2 | 2011-12-01 | 2012-01-03 |
NCT00849966 | Tonsillectomy|Adenotonsillectomy|Pain, Postoperative | Drug: Celebrex suspension|Drug: Placebo | Children's Hospital of Eastern Ontario|University of Ottawa | Phase 2 | 2009-08-01 | 2013-04-17 |
NCT00030420 | Lung Cancer | Drug: Celecoxib|Drug: Docetaxel | Barbara Ann Karmanos Cancer Institute|National Cancer Institute (NCI) | Phase 2 | 2001-10-01 | 2013-04-25 |
NCT00520338 | Postoperative Pain|Thyroidectomy|Cyclooxygenase 2 Inhibitors | Drug: celecoxib | Mahidol University | Phase 4 | 2007-08-01 | 2010-11-06 |
NCT00447759 | Osteoarthritis|Rheumatoid Arthritis | Drug: Celecoxib|Drug: non-selective Non steroidal anti inflammatory Drug | University of Dundee|University of Glasgow|University of Nottingham | Phase 4 | 2007-06-01 | 2016-01-07 |
NCT00571701 | Recurrent Respiratory Papillomatosis | Drug: celebrex (celecoxib)|Drug: placebo | Northwell Health|National Institute on Deafness and Other Communication Disorders (NIDCD)|University of Iowa|Eastern Virginia Medical School|University of Alabama at Birmingham|University of California, San Francisco|Vanderbilt University|Sanford Health|Weill Medical College of Cornell University | Phase 2 | 2008-02-01 | 2016-12-29 |
NCT00585156 | Bone Ingrowth|Pain | Drug: Celecoxib | University of Utah|Pfizer | Early Phase 1 | 2008-06-01 | 2016-03-11 |
NCT02876094 | Spinal Muscular Atrophy (SMA) | Drug: celecoxib | Hugh McMillan|Families of SMA Canada|Gwendolyn Strong|Children's Hospital of Eastern Ontario | Phase 2 | 2016-09-01 | 2016-09-16 |
NCT01901679 | Obesity | Drug: Celebrex | Rockefeller University | Early Phase 1 | 2013-07-01 | 2014-11-04 |
NCT00087256 | Colorectal Cancer | Drug: Celecoxib|Other: placebo | NSABP Foundation Inc|National Cancer Institute (NCI) | Phase 3 | 2004-07-01 | 2013-01-04 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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