| 应用 |
A reversible antagonist of the platelet purinergic P2Y12 receptor |
| 产品介绍 |
Ticagrelor (替格瑞洛; AZD-6140) 是第一个结合可逆的口服P2Y12受体拮抗剂，Ki为2 nM，还能抑制CYP2C9，IC50为10.5 μM。 |
| 生化机理 |
Ticagrelor is an active drug which, does not require metabolic activation after intestinal absorption. It does not compete directly with ADP at the ADP binding site but occupies an adjacent binding site and acts in an allosteric way, resulting in a reversible conformational change of the receptor. Ticagrelor binds reversibly to the receptor and exhibits rapid onset and offset of effect. Binding studies in rh-P2Y12 receptor-transfected CHO-K1 cells indicate that ticagrelor exhibits potent, rapid, and reversible binding, with a Kd of 10.5 nM, a kon (association constant) of 0.00011/(nM?s), a koff (dissociation constant) of 0.00087/s, and half-life values of 4 min for binding and 14 min for unbinding, indicating that the magnitude of platelet inhibition is dependent on concentrations of drug available to bind platelets. |
| 别名 |
替卡格雷;替格瑞洛;AR-C 126532XX; AZD 6140;AZD6140;AZD-6140;(1S,2S,3R,5S)-3-[7-[[(1R,2S)-2-(3,4-Difluorophenyl)cyclopropyl]amino]-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)-1,2-cyclopentanediol |
