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CAS No.: 78712-43-3

盐酸奥扎格雷 Catalog No. CSN16785

Synonyms: OKY-046 hydrochloride;OKY-046 HCl

Ozagrel HCl is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.

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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]. Ozagrel Hydrochloride is the hydrochloride form of Ozagrel. 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].
参考文献

[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.
[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
- 3.7778 mL
- 18.8888 mL
- 37.7775 mL
- 5 mM
- 0.7556 mL
- 3.7778 mL
- 7.5555 mL
- 10 mM
- 0.3778 mL
- 1.8889 mL
- 3.7778 mL

技术信息

CAS号

78712-43-3

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H13ClN2O2

运输

蓝冰

分子量

264.71

别名

OKY-046 hydrochloride;OKY-046 HCl

溶解度

DMSO	52.0 mg/mL (196.4 mM)
Water	51.0 mg/mL (192.7 mM)
Ethanol	6.0 mg/mL (22.7 mM)

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