同义名 :	OKY-046
	CAS号 :	82571-53-7
	货号 :	A130858
	分子式 :	C13H12N2O2
	纯度 :	98%
	分子量 :	228.25
	MDL号 :	MFCD00868231
	存储条件：	Pure form Sealed in dry,2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

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].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	4.38mL 0.88mL 0.44mL	21.91mL 4.38mL 2.19mL	43.81mL 8.76mL 4.38mL

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. 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