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CAS No.: 82571-53-7

Ozagrel/奥扎格雷 Catalog No. CSN16475

Synonyms: OKY-046;KCT-0809;Cataclot

Ozagrel is an antiplatelet agent working as a thromboxane A2 synthesis inhibitor.

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生物活性

实验方案

技术信息

生物活性

描述TXA₂ (thromboxane A₂) is known as a potent vasoconstrictive eicosanoid that can modulate pulmonary arterial pressure and hypoxic pulmonary vasoconstriction. TXA₂ is involved in the early phases of oleic acid (OA)–induced lung injury, a representative model of ARDS/ALI (acute respiratory distress syndrome/acute lung injury)^[3]. TXA₂ synthase activity was selectively inhibited by Ozagrel and its IC₅₀ for the rabbit platelet enzyme was found to be 11nM^[4]. To evaluate efficacy, 80 mg/kg ozagrel was administered intravenously 30 min prior to OA injection. Administration of ozagrel prevented an increase in expression of MCP-1 and IL-8 mRNA in whole lungs 3 h after OA injection. There was a significant decrease in the MCP-1/β-actin and IL-8/β-actin ratios in the OA + ozagrel group compared with the OA + saline group. Moreover, Ozagrel significantly inhibited the increase in TXB₂ levels in BALF 1.5 h after OA injection. These results indicated that ozagrel reduces pulmonary vascular hyper-permeability, the inflammation that is manifested by infiltration of macrophages and neutrophils, and the over-expression of MCP-1 and IL-8 mRNA in lungs induced by OA injection^[3].
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
NCT00200356 Cerebral Infarction Phase 4 Completed - -
NCT00200356 - - Completed - -
参考文献

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00200356	Cerebral Infarction	Phase 4	Completed	-	-
NCT00200356	-	-	Completed	-	-

[1] Ishitsuka Y, Moriuchi H, et al. A selective thromboxane A2 (TXA2) synthase inhibitor, ozagrel, attenuates lung injury and decreases monocyte chemoattractant protein-1 and interleukin-8 mRNA expression in oleic acid-induced lung injury in guinea pigs. J Pharmacol Sci. 2009 Oct;111(2):211-5. Epub 2009 Sep 26.
[2] Imamura T, Kiguchi S, et al. Effect of ozagrel, a selective thromboxane A2-synthetase inhibitor, on cerebral infarction in rats. Comparative study with norphenazone, a free-radical scavenger. Arzneimittelforschung. 2003;53(10):688-94.
[3] A selective thromboxane A2 (TXA2) synthase inhibitor, ozagrel, attenuates lung injury and decreases monocyte chemoattractant protein-1 and interleukin-8 mRNA expression in oleic acid-induced lung injury in guinea pigs
[4] Effects of thromboxane synthetase inhibitors on aggregation of rabbit platelets

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.3812 mL
- 21.9061 mL
- 43.8123 mL
- 5 mM
- 0.8762 mL
- 4.3812 mL
- 8.7625 mL
- 10 mM
- 0.4381 mL
- 2.1906 mL
- 4.3812 mL

技术信息

CAS号

82571-53-7

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H12N2O2

运输

蓝冰

分子量

228.25

别名

OKY-046;KCT-0809;Cataclot;Xanbo;奥扎格雷

溶解度

DMSO	46.0 mg/mL (201.5 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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Ozagrel/奥扎格雷 Catalog No. CSN16475

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