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/ Valdecoxib

伐地考昔 /Valdecoxib {[allProObj[0].p_purity_real_show]}

货号：A727456 同义名： 代他考昔 / SC 65872

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

Valdecoxib 化学结构 CAS号：181695-72-7
Valdecoxib 化学结构
CAS号：181695-72-7
Valdecoxib 3D分子结构
CAS号：181695-72-7
Valdecoxib 化学结构 CAS号：181695-72-7
Valdecoxib 3D分子结构 CAS号：181695-72-7
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Valdecoxib 纯度/质量文件 产品仅供科研

货号：A727456 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。

Valdecoxib 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].

Valdecoxib 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 <<

Valdecoxib 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

Valdecoxib 实验方案

计算器
存储液制备 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

Valdecoxib 技术信息

CAS号181695-72-7
分子式C16H14N2O3S
分子量 314.359
别名 代他考昔 ;SC 65872
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature
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

Tags: Valdecoxib | 181695-72-7 | SC 65872 | SC65872 | SC-65872 | COX-2 Inhibitor | Immunology/Inflammation | Metabolic Enzyme/Protease | COX | Endogenous Metabolite | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Valdecoxib 纯度/质量文件 | Valdecoxib 亚型比较 | Valdecoxib 生物活性 | Valdecoxib 临床数据 | Valdecoxib 参考文献 | Valdecoxib 实验方案 | Valdecoxib 技术信息

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