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/ 环氧化酶 / Lumiracoxib

罗美昔布 /Lumiracoxib {[allProObj[0].p_purity_real_show]}

货号：A112255 同义名： COX-189

Lumiracoxib is a COX2 selective inhibitor and a non-steroidal anti-inflammatory drug (NSAID), which inhibits COX2 with IC50 and Ki values of 0.14 μM and 0.06 μM and inhibits COX1 with Ki of 3 μM.

Lumiracoxib 化学结构 CAS号：220991-20-8
Lumiracoxib 化学结构
CAS号：220991-20-8
Lumiracoxib 3D分子结构
CAS号：220991-20-8
Lumiracoxib 化学结构 CAS号：220991-20-8
Lumiracoxib 3D分子结构 CAS号：220991-20-8
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Lumiracoxib 纯度/质量文件 产品仅供科研

货号：A112255 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。

Lumiracoxib 生物活性

靶点

  • COX-2

    COX-2, Ki:60 nM

  • COX-1

    COX-1, Ki:3 μM
描述 Lumiracoxib is a selective cyclooxygenase (COX)-2 inhibitor that possesses a carboxylic acid group that makes it weakly acidic. It has good oral bioavailability; maximum plasma concentrations are reached two hours after oral administration. Lumiracoxib has been found to be effective at doses of 100 - 400 mg once a day for chronic pain and 400 mg/day for acute pain. In comparison to NSAIDs (nonsteroidal anti-inflammatory drugs), patients taking lumiracoxib experience significantly fewer adverse events and greater tolerability[3]. In single- and multiple-dose well designed trials in patients with acute pain associated with primary dysmenorrhoea, dental or orthopaedic surgery or tension-type headache, lumiracoxib 100 - 800 mg once daily was more effective in relieving acute pain than placebo or controlled-release oxycodone 20 mg, and was at least as effective as selective COX-2 inhibitors or nonselective NSAIDs[4]. COX-2 selectivity of lumiracoxib is associated with a reduced incidence of gastroduodenal erosions compared with naproxen and a lack of effect on both small and large bowel permeability[5].

Lumiracoxib 参考文献

[1]Dickie AP, Wilson CE, et al. The pharmacokinetics and metabolism of lumiracoxib in chimeric humanized and murinized FRG mice. Biochem Pharmacol. 2017 Jul 1;135:139-150.

[2]Esser R, Berry C, et al. Preclinical pharmacology of lumiracoxib: a novel selective inhibitor of cyclooxygenase-2. Br J Pharmacol. 2005 Feb;144(4):538-50.

[3]Buvanendran A, Barkin R. Lumiracoxib. Drugs Today (Barc). 2007;43(3):137-147

[4]Lyseng-Williamson KA, Curran MP. Lumiracoxib. Drugs. 2004;64(19):2237-2248

[5]Rordorf CM, Choi L, Marshall P, Mangold JB. Clinical pharmacology of lumiracoxib: a selective cyclo-oxygenase-2 inhibitor. Clin Pharmacokinet. 2005;44(12):1247-1266

Lumiracoxib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.40mL

0.68mL

0.34mL

17.02mL

3.40mL

1.70mL

34.05mL

6.81mL

3.40mL

Lumiracoxib 技术信息

CAS号220991-20-8
分子式C15H13ClFNO2
分子量 293.721
别名 COX-189
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,Store in freezer, under -20°C
溶解度

DMSO: 120 mg/mL(408.55 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

Tags: Lumiracoxib | COX-189 | COX | AmBeed-信号通路专用抑制剂 | Lumiracoxib 纯度/质量文件 | Lumiracoxib 亚型比较 | Lumiracoxib 生物活性 | Lumiracoxib 参考文献 | Lumiracoxib 实验方案 | Lumiracoxib 技术信息

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