产品说明书

Celecoxib

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Chemical Structure| 169590-42-5 同义名 : 塞来西布 ;SC 58635;YM-177;Celebrex
CAS号 : 169590-42-5
货号 : A180379
分子式 : C17H14F3N3O2S
纯度 : 98%
分子量 : 381.37
MDL号 : MFCD00941298
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(131.11 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：

2% DMSO+30% PEG 300+5% Tween 80+water 5 mg/mL

生物活性
靶点

  • COX-2

    COX-2, IC50:40 nM
描述 Cyclooxygenase (COX) is an enzyme that produces precursors to prostaglandins and thromboxanes. It is associated with rheumatoid arthritis (RA), osteoarthritis (OA), and other inflammatory disorders. Celecoxib is a dyaryl heterocyclic inhibitor of COX-2, a subtype of COX that is highly expressed in inflamed tissues. In human dermal fibroblasts, celecoxib inhibited COX-2-mediated production of prostaglandin E2 (PGE2) with an IC50 at 91 nM, compared to its IC50 value of COX-1 inhibition at 2800 nM[6]. When IL-1β-stimulated fibroblast-like synoviocytes were treated by 10 μM celecoxib for 24 hours, the production of PGE2 and the gene expression of COX-2 were significantly decreased compared to non-treated cells[7]. In vivo, celecoxib was orally administrated to male Sprague-Dawley rats 4 hours after carrageenan injection, and it was shown to abrogate carrageenan-induced thermal hyperalgesia with an ED30 value of 0.81 mg/kg. Celecoxib also showed inhibitory effect on lipopolysaccharide-induced pyrexia in rats with an ED30 of 1.3 mg/kg[6]. RA patients who received 40, 200, or 400 mg celecoxib twice daily for 4 weeks presented significantly reduced signs and symptoms[8]. In OA patients, 6-week treatment of 200 mg celecoxib once daily significantly improved their scores on pain satisfaction scales[9].
作用机制 The phenylsulfonamide moiety of celecoxib binds to the side pocket of cyclooxygenase (COX)-2 to prevent the activation of COX-2 to other stimuli[8].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
201T Growth Inhibition Assay 72 h IC50=48.6 µM 25057941
273T Growth Inhibition Assay 72 h IC50=80.5 µM 25057941
A2780 5/10/15 μM Function Assay 48 h decreases Cox-2 expression in a dose-dependent manner 25424898
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
NCT00653250 Lung Cancer Not Applicable Completed - -
NCT00533247 Postoperative Pain Not Applicable Unknown - Canada, British Columbia ... 展开 >> Not yet recruiting Vancouver, British Columbia, Canada Contact: Adam Zanbilowicz, BA DPM MS    604-885-8803    zanbilowicz@pol.net 收起 <<
NCT00153660 Arthritis Car... 展开 >>diovascular Diseases Cerebrovascular Disorders 收起 << Phase 3 Completed - China, Hong Kong ... 展开 >> Endoscopy Center, Prince of Wales Hospital Shatin, Hong Kong, China 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.62mL

0.52mL

0.26mL

13.11mL

2.62mL

1.31mL

26.22mL

5.24mL

2.62mL
参考文献

[1]Safaeian L, Hajhashemi V, et al. The effect of celecoxib on blood pressure and plasma oxidant/antioxidant status in co-administration with glucocorticoid in rat. Biomed Pharmacother. 2018 Dec;108:1804-1808.

[2]Paulson SK, Vaughn MB, et al. Pharmacokinetics of celecoxib after oral administration in dogs and humans: effect of food and site of absorption. J Pharmacol Exp Ther. 2001 May;297(2):638-45.

[3]CELEBREX

[4]55(7):394-402.

[5]42(6):499-506.

[6]Yoshino T, Kimoto A, Kobayashi S, Noguchi M, Fukunaga M, Hayashi A, Miyata K, Sasamata M. Pharmacological profile of celecoxib, a specific cyclooxygenase-2 inhibitor. Arzneimittelforschung. 2005;55(7):394-402.

[7]Kawashima M, Ogura N, Akutsu M, Ito K, Kondoh T. The anti-inflammatory effect of cyclooxygenase inhibitors in fibroblast-like synoviocytes from the human temporomandibular joint results from the suppression of PGE2 production. J Oral Pathol Med. 2013 Jul;42(6):499-506.