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/ Celecoxib

塞来昔布 /Celecoxib {[allProObj[0].p_purity_real_show]}

货号：A180379 同义名： 塞来西布 / SC 58635;YM-177

Celecoxib is a selective COX-2 inhibitor with IC50 of 40 nM.

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Celecoxib 化学结构 CAS号：169590-42-5
Celecoxib 化学结构
CAS号：169590-42-5
Celecoxib 3D分子结构
CAS号：169590-42-5
Celecoxib 化学结构 CAS号：169590-42-5
Celecoxib 3D分子结构 CAS号：169590-42-5
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Celecoxib 纯度/质量文件 产品仅供科研

货号：A180379 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 COX ↓ COX-1 ↓ COX-2 ↓ 其他靶点 纯度
Piroxicam ✔ 98%
Salicylic acid ✔ 98%
Phenacetin ✔ 98%
Etodolac ✔ 99%
Flunixin meglumine ✔ 98%
Ibuprofen L-lysine ✔ 99%
Nabumetone ✔ 98%
Acemetacin ✔ 98%
Diflunisal ✔ 98%
Pranoprofen ✔ 98%
Ampiroxicam ✔ 98%
Meloxicam ✔ 98%
Sulindac ✔ 98%
Ketoprofen ✔ 98%
Mefenamic Acid ✔ 95%
Bromfenac sodium ✔ 98%
Oxaprozin ✔ 99%
Aspirin ✔ 99%
Nepafenac ✔ 98%
Zaltoprofen ✔ 99%
Salicin ✔ 98%
Suprofen ✔ 99%+
Xanthohumol ✔ 99%
Parecoxib ✔ 98%
Tolfenamic Acid +++

COX-2, IC50: 0.2 μM

 		98%
Etoricoxib ✔ 99%
Niflumic Acid ✔ 98%
Valdecoxib ++++

COX-2, IC50: 5 nM

 		99+%
Ibuprofen +

COX-1, IC50: 13 μM

 		+

COX-2, IC50: 370 μM

 		98%
Indomethacin ++

COX1, IC50: 0.28 μM

 		+

COX-2, IC50: 14 μM

 		97%
Lornoxicam ++++

COX-1, IC50: 5 nM

 		++++

COX-2, IC50: 8 nM

 		98%
Meclofenamic acid sodium ++++

COX-1, IC50: 40 nM

 		+++

COX-2, IC50: 50 nM

 		99%
Rofecoxib ++++

COX-2, IC50: 18 nM

 		98%
Asaraldehyde ✔ 98%
Naproxen +

COX-1, IC50: 8.7 μM

 		+

COX-2, IC50: 5.2 μM

 		98%
Diclofenac Sodium Salt +++

COX-1, IC50: 60 nM

 		+++

COX-2, IC50: 200 nM

 		98%
NS-398 ++

COX-2, IC50: 3.8 μM

 		98%
Amfenac Sodium Hydrate ++

COX-1, IC50: 250 nM

 		+++

COX-2, IC50: 150 nM

 		98%+
Nimesulide +

COX-2, IC50: 26 μM

 		98%
Lumiracoxib ++

COX-1, Ki: 3 μM

 		+++

COX-2, Ki: 60 nM

 		98%
Rutaecarpine ✔ 95%
Celecoxib ++++

COX-2, IC50: 40 nM

 		98%
Carprofen ++++

canine COX2, IC50: 30 nM

 		98%
Ketorolac ++

COX-1 (human), IC50: 1.23 μM

 		++

COX-2 (human), IC50: 3.50 μM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Celecoxib 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].

Celecoxib 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
A2780 5/10/15 μM Function Assay 48 h elevates the expression of E-cadherin and keratin 25424898

Celecoxib 动物研究

Dose Rat: 10 mg/kg - 50 mg/kg[3] (p.o.) Dog: 7.5 mg/kg - 25 mg/kg[4] (p.o.)
Administration p.o.
Pharmacokinetics
Animal Rats[5]
Dose 10 mg/kg
Administration p.o./i.v.
F 64.5% (p.o.)
Vd 1860 ml/kg (i.v.)
T1/2 3.67 h (p.o.)
3.49 h (i.v.)
Tmax 3 h (p.o.)
Cmax 2.01 μg/ml (p.o.)
4.87 μg/ml (i.v..)
AUC0→∞ 18.5 μg·h/ml (p.o.)
28.7 μg·h/ml (i.v.)

Celecoxib 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 <<

Celecoxib 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.

Celecoxib 实验方案

计算器
存储液制备 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

Celecoxib 技术信息

CAS号169590-42-5
分子式C17H14F3N3O2S
分子量 381.37
别名 塞来西布 ;SC 58635;YM-177;Celebrex
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature
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

Tags: Celecoxib | 169590-42-5 | SC 58635 | SC58635 | SC-58635 | COX-2inhibitor | Immunology/Inflammation | COX | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Celecoxib 纯度/质量文件 | Celecoxib 亚型比较 | Celecoxib 生物活性 | Celecoxib 细胞研究 | Celecoxib 动物研究 | Celecoxib 临床数据 | Celecoxib 参考文献 | Celecoxib 实验方案 | Celecoxib 技术信息

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