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/ Etoricoxib

依托考昔 /Etoricoxib 99%

货号：A137375 同义名： MK-0663;L-791456 Ambeed 开学季，买赠积分，赢豪礼

Etoricoxib is a selective COX2 inhibitor with IC50 of 1.1 ± 0.1 μM and 116 ± 8 μM for COX1.

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Etoricoxib 化学结构 CAS号：202409-33-4
Etoricoxib 化学结构
CAS号：202409-33-4
Etoricoxib 3D分子结构
CAS号：202409-33-4
Etoricoxib 化学结构 CAS号：202409-33-4
Etoricoxib 3D分子结构 CAS号：202409-33-4
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Etoricoxib 纯度/质量文件 产品仅供科研

货号：A137375 标准纯度： 99%
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。

Etoricoxib 生物活性

靶点

  • COX-2
描述 Etoricoxib is a novel orally active agent that selectively inhibits cyclooxygenase-2 (COX-2). Etoricoxib is a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM, 116 μM and 5 μM for COX-2, COX-1 in human whole blood and purified human COX-2, respectively. Etoricoxib shows inhibitory effect on PGE2 production by CHO (COX-2) cells (IC50, 79 nM), on purified human COX-2 with detergent (IC50, 4.1 μM), and on purified PGE2 production by U937 microsomes (low substrate; IC50, 12.1 μM). However, Etoricoxib has little activity against COX-1 with a Ki of 167 μM[3]. Etoricoxib in 50 and 100 mg/kg doses changed the levels of oxidant/antioxidant parameters such as MDA, MPO, tGSH, GSHRd, GST, SOD, NO, and 8-OH/Gua in favour of antioxidants. Furthermore, etoricoxib prevented increase of COX-2 gene expression and ALT and AST levels[4]. Etoricoxib 120 mg administered orally once daily has the same efficacy on acute gout as indometacin and diclofenac. Etoricoxib is tolerated better by patients than NSAIDs such as indometacin and diclofenac[5].

Etoricoxib 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
NCT01638962 Osteoarthritis, Knee Not Applicable Completed - Denmark ... 展开 >> University of Southern Denmark Odense, Region Syddanmark, Denmark, 5230 收起 <<
NCT00092729 Dysmenorrhea Phase 3 Completed - -
NCT03117894 Breast Neoplasm Female ... 展开 >> Regional Anesthesia Anesthesia Regional Anesthesia Morbidity Anesthesia Morbidity 收起 << Not Applicable Unknown December 2018 Sweden ... 展开 >> Östersund Hospital Recruiting Östersund, Jämtland, Sweden, 83183 Contact: Hans Ahlberg, MD    +4663153000    hans.ahlberg@regionjh.se    Contact: Joakim Johansson, PhD    +46703976410    joakim.johansson@regionjh.se 收起 <<

Etoricoxib 参考文献

[1]Jayaraman R, Manisenthil KT, et al. Influence of etoricoxib on anticonvulsant activity of phenytoin and diazepam in experimental seizure models in mice. J Pharm Pharmacol. 2010 May;62(5):610-4.

[2]Schiffmann S, Sandner J, et al. The selective COX-2 inhibitor celecoxib modulates sphingolipid synthesis. J Lipid Res. 2009 Jan;50(1):32-40.

[3]Riendeau D, Percival MD, Brideau C, et al. Etoricoxib (MK-0663): preclinical profile and comparison with other agents that selectively inhibit cyclooxygenase-2. J Pharmacol Exp Ther. 2001;296(2):558-566

[4]Kunak CS, Kukula O, Mutlu E, et al. The Effect of Etoricoxib on Hepatic Ischemia-Reperfusion Injury in Rats. Oxid Med Cell Longev. 2015;2015:598162

[5]Zhang S, Zhang Y, Liu P, Zhang W, Ma JL, Wang J. Efficacy and safety of etoricoxib compared with NSAIDs in acute gout: a systematic review and a meta-analysis. Clin Rheumatol. 2016;35(1):151-158

Etoricoxib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.79mL

0.56mL

0.28mL

13.93mL

2.79mL

1.39mL

27.87mL

5.57mL

2.79mL

Etoricoxib 技术信息

CAS号202409-33-4
分子式C18H15ClN2O2S
分子量 358.842
别名 MK-0663;L-791456;Etoricoxib, Arcoxia, L-791456, MK 0663, MK-0663;Nucoxia;Algix;Tauxib;MK-663;Arcoxia
运输蓝冰
存储条件

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 105 mg/mL(292.61 mM)，配合低频超声助溶，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

IP 2% DMSO+2% Tween80+40% PEG300+water 10 mg/mL clear

PO 0.5% CMC-Na 65 mg/mL suspension

Tags: Etoricoxib | 202409-33-4 | MK-0663 | L-791456 | MK0663 | MK 0663 | L791456 | L 791456 | L-791456 | COX Inhibitor | Immunology/Inflammation | COX | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Etoricoxib 纯度/质量文件 | Etoricoxib 亚型比较 | Etoricoxib 生物活性 | Etoricoxib 临床数据 | Etoricoxib 参考文献 | Etoricoxib 实验方案 | Etoricoxib 技术信息

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