| Description | Prasugrel (CS-747) is a piperazine derivative and PLATELET AGGREGATION INHIBITOR that is used to prevent THROMBOSIS in patients with ACUTE CORONARY SYNDROME; UNSTABLE ANGINA and MYOCARDIAL INFARCTION, as well as in those undergoing PERCUTANEOUS CORONARY INTERVENTIONS. |
| In vitro | 0.3-3 mg/kg Prasugrel在栓塞性脑梗死大鼠模型中,剂量依赖性减少血管损伤24小时后脑梗塞的发病率.月桂酸诱导大鼠外周血管闭塞性疾病,月桂酸注射前每天给药0.03-3 mg/kg Prasugrel,连续给药11天,可以剂量依赖性抑制疾病的发展. 一天一次,连续14天,对狗每天给药0.03-3 mg/kg ,对猴子每天给药0.1-0.3 mg/kg Prasugrel,能够剂量相关性和累加性抑制ADP诱导的血小板聚集.给电诱导动脉血栓形成的大鼠模型每天口服0.1-1 mg/kg Prasugrel,可以明显延长动脉闭塞时间,并提高动脉通畅率.Prasugrel在WT小鼠体内表现出血小板抑制作用,比氯吡格雷有效8.2倍. |
| In vivo | Prasugrel比氯吡格雷具有更快,更高和更可靠的血小板聚集抑制作用,它在体内代谢为活性代谢物,具有选择性P2Y(12)拮抗活性。 |
| Target activity | Platelet:1.8 μM |
| Synonyms | LY640315, CS-747, 普拉格雷, PCR 4099 |
| molecular weight | 373.44 |
| Molecular formula | C20H20FNO3S |
| CAS | 150322-43-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 45 mg/mL (120.5 mM) |
| References | 1. Hashimoto M, et al. Biochem Pharmacol, 2007, 74(7), 1003-1009. 2. Ogawa T, et al. Eur J Pharmacol, 2009, 612(1-3), 29-34. 3. Niitsu Y, et al. Eur J Pharmacol, 2008, 579(1-3), 276-282. |