帕瑞昔布钠

中文名称:

帕瑞昔布钠

中文同义词:

帕瑞考昔钠;帕瑞昔布钠杂质(4个);帕瑞昔布钠;帕瑞西布纳原料药;帕瑞昔布(钠盐);N-[[4-(5-甲基-3-苯基-4-异恶唑基)苯基]磺酰]丙酰胺钠盐(帕来昔布钠);帕瑞昔布杂质25;帕瑞西布钠

英文名称:

PARECOXIB SODIUM

英文同义词:

Parecoxib sodium （Intermediate in China ONLY）;N-[4-(5-METHYL-3-PHENYLISOXAZOL-4-YL)PHENYLSULFONYL]PROPIONAMIDE, SODIUM SALT;Parecoxib sodiuM salt;Dynastat;N-[[4-(5-Methyl-3-phenyl-4-isoxazolyl)phenyl]sulfonyl]propanaMide SodiuM Salt;Rayzon;SC 69124A;PropanaMide,N-[[4-(5-Methyl-3-phenyl-4-isoxazolyl)phenyl]sulfonyl]-, sodiuM salt (1:1)

CAS号:

198470-85-8

分子式:

C19H17N2NaO4S

分子量:

392.40405

EINECS号:

813-689-5

相关类别:

帕瑞考昔钠;原料药;医药原料药;医药原料;医药中间体;消炎镇痛;杂质对照品;Aromatics;Heterocycles;Intermediates Fine Chemicals;Pharmaceuticals;对照品-杂质对照品;医药化工类;医用原料;科研试剂;药物杂质及中间体;化工原料药;原料;化工原料

Mol文件:

198470-85-8.mol

熔点 

273-275°C

储存条件 

Inert atmosphere,2-8°C

用途

帕瑞昔布钠药物对于疼痛,炎症和发热问题会有很大的帮助,可以选择性抑制降低组织包括内皮组织前列腺素的形成,不过对于血小板血栓烷素没有影响。帕瑞昔布钠在临床上一般用于中度或者重度手术后的急性疼痛的治疗。

作用

帕瑞昔布钠具有抗炎，止痛的作用。

生物活性

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。

靶点

COX-2

COX-2

体外研究

Parecoxib Sodium (0-200 μM; 24-48 hours) inhibits the cell proliferation of GBM cells in a dose-dependent manner in GBM cells.Parecoxib Sodium (200 μM; 24-48 hours) results in a decreased migratory ability of U343 cells than PBS-treated group. Cell Viability Assay 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.

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

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. Animal Model: Naive adult male ICR mice, 15 weeks old and weighing 25-35 g 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.

Animal Model:

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

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.

用途 

全球第一个可静脉给药和肌肉注射的特异性环氧合酶-2（COX-2）抑制剂，用于手术后疼痛的短期治疗，也可用于中度或重度术后急性疼痛的治疗