Parecoxib(Synonyms: 帕瑞昔布; SC 69124)

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Parecoxib (Synonyms: 帕瑞昔布; SC 69124) 纯度: 98.34%

Parecoxib (SC 69124) 是一种选择性强、口服活性强的 COX-2 抑制剂，Valdecoxib (HY-15762) 的前药。Parecoxib Sodium 是一种非甾体抗炎试剂 (NSAID)，可抑制前列腺素(PG) 的合成。动物实验中，Parecoxib Sodium 可用于缓解术后急性疼痛和骨关节炎、类风湿关节炎等慢性炎症症状。

Parecoxib(Synonyms: 帕瑞昔布; SC 69124)

Parecoxib Chemical Structure

CAS No. : 198470-84-7

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥770 In-stock
25 mg ￥700 In-stock
50 mg ￥1200 In-stock
100 mg ￥2000 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

Parecoxib (SC 69124) is a highly selective and orally active COX-2 inhibitor, the prodrug of Valdecoxib (HY-15762). Parecoxib Sodium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits prostaglandin (PG) synthesis. Parecoxib can be used for the relief of acute postoperative pain and symptoms of chronic inflammatory conditions such as osteoarthritis and rheumatoid arthritis in vivo[1][2].

IC50 & Target[1]

COX-2

 

体外研究
(In Vitro)

Parecoxib (0-200 μM; 24-48 hours) inhibits the cell proliferation of GBM cells in a dose-dependent manner in GBM cells[4].
Parecoxib (200 μM; 24-48 hours) results in a decreasee migratory ability of U343 cells than PBS-treated group[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[4]

Cell Line: GBM cells: U251 and U343 cells
Concentration: 0 μM, 20 μM, 50 μM, 100 μM and 200 μM
Incubation Time: 24-48 hours
Result: Resulted in a slower BrdU incorporation rate of GBM cells including U251 and U343 cells.

体内研究
(In Vivo)

Parecoxib (intraperitoneal injection; 2.5, 5.0 or 10 mg/kg; once a day; 21 days) does not affect locomotor activity in the elevated plus-maze test, and Parecoxib at 5 and 10 mg/kg shows higher levels of percentage of time spent in the open arms[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Naive adult male ICR mice, 15 weeks old and weighing 25-35 g[3]
Dosage: 2.5, 5.0 or 10 mg/kg
Administration: Intraperitoneal injection; 2.5, 5.0 or 10 mg/kg; once a day; 21 days
Result: Exerted an anxiolytic-like effect in the elevated plus-maze test

Clinical Trial

分子量

370.42

Formula

C19H18N2O4S
CAS 号

198470-84-7
中文名称

帕瑞昔布；帕瑞考昔
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 50 mg/mL (134.98 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6996 mL 13.4982 mL 26.9964 mL
5 mM 0.5399 mL 2.6996 mL 5.3993 mL
10 mM 0.2700 mL 1.3498 mL 2.6996 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制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

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.75 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.75 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.75 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.75 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Jun Tang, et al. Effect of parecoxib, a novel intravenous cyclooxygenase type-2 inhibitor, on the postoperative opioid requirement and quality of pain control. Anesthesiology

    [2]. J L Mateos, et al.[Selective inhibitors of cyclooxygenase-2 (COX-2), celecoxib and parecoxib: a systematic review]. Drugs Today (Barc). 2010 Feb;46 Suppl A:1-25.

    [3]. Bo Wang, et al. Chronic administration of parecoxib exerts anxiolytic-like and memory enhancing effects and modulates synaptophysin expression in mice. BMC Anesthesiol. 2017 Nov 13;17(1):152.

    [4]. Lin-Yong Li, et al. Parecoxib inhibits glioblastoma cell proliferation, migration and invasion by upregulating miRNA-29c. Biol Open. 2017 Mar 15;6(3):311-316.

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