Ticagrelor (AZD6140) 是可逆的，可口服的P2Y12受体拮抗剂，可抑制血小板聚集。

Ticagrelor, produced by AstraZeneca, is an inhibitor of platelet aggregation. Unlike clopidogrel, ticagrelor is not a prodrug required metabolic activation. The drug was approved for use in the European Union by the European Commission on December 3, 2010, and by the US FDA on July 20, 2011. Its trade names are Brilinta (US), Brilique(EU) and Possia(EU).

Ticagrelor的t1/2大约为7-8.5小时.Ticagrelor与血小板聚集的抑制剂量有关,以100-400 mg处理2小时可完全抑制.Ticagrelor有良好的耐受性,既无严重的不良事件,也无明显的实验值变化.Ticagrelor吸收快,1.3-2小时即可达峰.在所研究的剂量范围内,Ticagrelor峰值浓度和药时曲线下面积（从时间0到无穷大的）以明显的剂量比例增加,表明其线性药物动力学特征.

在对rh-P2Y12受体转染的CHO-K1进行结合研究中,Ticagrelor表现出高效可逆的结合,kon(结合常数)为0.00011/(nM·s),Kd为10.5 nM,koff(解离常数)为0.00087/s,结合与解离半衰期值分别为4分钟和14分钟,表明可结合血小板的药物浓度决定了血小板的抑制大小。Ticagrelor是不需要代谢活化的活性药物。Ticagrelor不与ADP在ADP结合位点直接竞争,但会占据邻近的结合位点,改变结合位点构象导致一个可逆的受体的构象变化。Ticagrelor与受体结合是可逆的,快速起/失效。

274693-27-5

C23H28F2N6O4S

522.57

替卡格雷;AR-C 126532XX;AZD6140

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years