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产品编号:  AD.Y00022-1kg 中文名称:  帕瑞昔布钠
中文别名:  帕瑞考昔钠 英文名称:  Parecoxib Sodium
英文别名:  Parecoxib sodiuM salt 品牌: ANDY
规格型号:  1kg CAS号:  198470-85-8
分子式:  C19H17N2NaO4S 分子量: 392.40
外观与性状:   储存条件: 2-8°C
纯度:  99%
标准价:  询价篮 优惠价:  暂无
数量:  

单位:  
库存与货期:  订货

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商品信息

Parecoxib Sodium (SC 69124A) 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。


生物活性

Parecoxib Sodium (SC 69124A) 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 Sodium 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 Sodium (0-200?μM; 24-48 hours) inhibits the cell proliferation of GBM cells in a dose-dependent manner in GBM cells[4].
Parecoxib Sodium (200?μM; 24-48 hours) results in a decreased migratory ability of U343 cells than PBS-treated group
[4].

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 Sodium (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]

Animal Model:

Naive adult male ICR mice, 15 weeks old and weighing 25-35 g[3]

Dosage:

2.5 mg/kg, 5.0  mg/kg 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

NCT Number

Sponsor

Condition

Start Date

Phase

NCT01843010

First Affiliated Hospital, Sun Yat-Sen University

Postoperative Pain Management, Pain Threshold, Shoulder Pain, Laparoscopies

May 2013

Phase 4

NCT01393925

First Affiliated Hospital, Sun Yat-Sen University

Anti-Inflammatory Agents, Non-Steroidal|Pain, Postoperative|Laparoscopy

July 2011

Not Applicable

NCT00346268

Pfizer

Pain, Postoperative

December 2006

Phase 4

分子量

392.40

Formula

C??H??N?NaO?S

CAS

198470-85-8

中文名称

帕瑞昔布钠

SMILES

CCC(N([Na])S(=O)(C1=CC=C(C2=C(C)ON=C2C3=CC=CC=C3)C=C1)=O)=O

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 : ≥ 100 mg/mL (254.84 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

2.5484 mL

12.7421 mL

25.4842 mL

5 mM

0.5097 mL

2.5484 mL

5.0968 mL

10 mM

0.2548 mL

1.2742 mL

2.5484 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 (6.37 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.37 mM,饱和度未知) 的澄清溶液。

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

2.请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.37 mM,饱和度未知) 的澄清溶液。

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 20% SBE-β-CD 生理盐水水溶液中,混合均匀。

3.请依序添加每种溶剂: 10% DMSO    90% corn oil

Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.37 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。

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。

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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