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/ Valdecoxib/伐地考昔

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

货号：A727456 同义名： 代他考昔 / SC 65872

Valdecoxib是一种强效 COX 抑制剂，选择性抑制 COX-2，IC50 值为 5 nM。

Valdecoxib/伐地考昔 化学结构 CAS号：181695-72-7
Valdecoxib/伐地考昔 化学结构
CAS号：181695-72-7
Valdecoxib/伐地考昔 3D分子结构
CAS号：181695-72-7
Valdecoxib/伐地考昔 化学结构 CAS号：181695-72-7
Valdecoxib/伐地考昔 3D分子结构 CAS号：181695-72-7
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Valdecoxib/伐地考昔 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 ✔ 98%
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%
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

 		95%
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/伐地考昔 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/伐地考昔 细胞实验

Cell Line
Concentration Treated Time Description References
Human platelets 0–100 μM Valdecoxib 25 minutes To assess the reversible inhibition of platelet Cox-1 activity by Valdecoxib, with an IC50 value of 28 μM Proc Natl Acad Sci U S A. 2001 Dec 4;98(25):14583-8.
Ovine cyclooxygenase-1 (oCox-1) 200 μM aspirin and 0–100 μM Valdecoxib 30 minutes To evaluate the antagonism of Valdecoxib against the irreversible inactivation of oCox-1 by aspirin, with an EC50 value of 13 μM Proc Natl Acad Sci U S A. 2001 Dec 4;98(25):14583-8.
R28 cells 1 and 5 μmol/L 4 hours Valdecoxib protects R28 cells from OGD/R injury by decreasing the cell apoptosis rate Int J Mol Sci. 2022 Oct 26;23(21):12983.

Valdecoxib/伐地考昔 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice C57BL6 wild-type mice Subcutaneous (P1-P6) and intraperitoneal (P7-P21) 10 mg/kg Daily administration from postnatal day 1 (P1) to day 21 (P21) To evaluate the effect of Valdecoxib on kidney development in mice. Results showed that Valdecoxib caused minimal changes in renal morphology, with kidney weight to body weight ratio similar to controls, and a significant reduction in glomerular diameter, but less severe than other COX-2 inhibitors (e.g., rofecoxib, etoricoxib, and lumiracoxib). Br J Pharmacol. 2011 Jul;163(5):927-36
Mice MPTP-induced Parkinson's disease model Oral 10, 30 or 50 mg/kg Once daily, starting two weeks before MPTP injection until the end of the experiment Valdecoxib alleviated the microglial activation, the loss of TH-positive cells and the decrease in open field and vertical activity. COX-2 deficiency attenuated MPTP-induced microglial activation, degeneration of TH-positive cells, and loss of coordination. J Neuroinflammation. 2006 Mar 27;3:6
Sprague-Dawley rats Retinal ischemia-reperfusion injury model Intravitreal injection 5 μM Single dose, observed for 3 days Valdecoxib attenuates IRI-induced retinal injury by inhibiting RGC apoptosis Int J Mol Sci. 2022 Oct 26;23(21):12983.

Valdecoxib/伐地考昔 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/伐地考昔 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/伐地考昔 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/伐地考昔 技术信息

CAS号181695-72-7
分子式C16H14N2O3S
分子量 314.36
SMILES Code O=S(C1=CC=C(C2=C(C)ON=C2C3=CC=CC=C3)C=C1)(N)=O
MDL No. MFCD00950568
别名 代他考昔 ;SC 65872
运输蓝冰
InChI Key LNPDTQAFDNKSHK-UHFFFAOYSA-N
Pubchem ID 119607
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, room temperature
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

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/伐地考昔 纯度/质量文件 | Valdecoxib/伐地考昔 亚型比较 | Valdecoxib/伐地考昔 生物活性 | Valdecoxib/伐地考昔 临床数据 | Valdecoxib/伐地考昔 参考文献 | Valdecoxib/伐地考昔 实验方案 | Valdecoxib/伐地考昔 技术信息

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