Ozagrel HCl

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Chemical Structure| 78712-43-3 同义名 : OKY-046 hydrochloride; OKY-046 HCl; Ozagrel hydrochloride
CAS号 : 78712-43-3
货号 : A138148
分子式 : C13H13ClN2O2
纯度 : 97%
分子量 : 264.71
MDL号 : MFCD06795644
存储条件：

Pure form Inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(944.44 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(377.78 mM)，配合低频超声助溶
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.78mL

0.76mL

0.38mL

18.89mL

3.78mL

1.89mL

37.78mL

7.56mL

3.78mL
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