| Description | Ozagrel hydrochloride (OKY-046 HCl) is a selective thromboxane A(2) synthetase inhibitor used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia. |
| In vitro | 3 mg/kg Ozagrel减少大鼠大脑中动脉局部缺血再灌注后皮层梗死的面积和体积.Ozagrel对微血栓形成大鼠模型中的神经缺陷也有抑制作用.Ozagrel在有意识的脑缺血再灌注小鼠模型中,改善退化的自发运动活性和运动协调梗阻.Ozagrel还可以防止豚鼠肺泡灌洗液中乳酸脱氢酶活性的增加.Ozagrel在豚鼠体内,防止油酸诱导的血栓素A(2)产生和随后支气管肺灌洗液中总蛋白质浓度和巨噬细胞与嗜中性粒细胞数量的增加,以及全肺中单核细胞趋化蛋白1与白介素-8 mRNA表达的增加.Ozagrel在猫体内,抑制脑缺血再灌注SHR模型中阻塞再灌注诱导的脑组织比重下降,并且在大脑中动脉闭塞再灌注后,恢复缺血后脑皮层PO(2)的减少.Ozagrel也会增加脑缺血再灌注后脑组织中6-keto-PGF(1alpha)（一种前列腺素I(2) (PGI(2))代谢物）的水平. |
| Target activity | TXA2 synthase:11 nM |
| Synonyms | Ozagrel HCl, 盐酸奥扎格雷, OKY-046 HCl |
| molecular weight | 264.71 |
| Molecular formula | C13H12N2O2·HCl |
| CAS | 78712-43-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 65 mg/mL (245.55 mM) H2O: 48 mg/mL (181.3 mM) Ethanol: 6 mg/mL (22.66 mM) |
| References | 1. Ishitsuka Y, et al. J Pharmacol Sci, 2009, 111(2), 211-215. 2. Imamura T, et al. Arzneimittelforschung, 2003, 53(10), 688-694. 3. Ichikawa K, et al. Pharmacology, 1999, 59(5), 257-265. 4. Ishitsuka Y, et al. J Pharm Pharmacol, 2004, 56(4), 513-520. 5. Naito J, et al. Eur J Pharmacol. 1983, 91(1), 41-48. |