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Ticagrelor

品牌 厂商性质 产地 货期
阿拉丁 生产商 上海 现货

在线咨询 询底价
产品参数
货号 CAS号 操作
T125095-250mg 274693-27-5 询底价
T125095-500mg 274693-27-5 询底价
T125095-1g 274693-27-5 询底价
T125095-25mg 274693-27-5 询底价
T125095-100mg 274693-27-5 询底价
产品介绍

  • 分子式 C23H28F2N6O4S
  • 分子量522.57

属性

沸点 ~777.6 °C at 760 mmHg
熔点 149-154 °C
折光率 1.74
溶解性
  • DMSO 105 mg/mL
  • Water <1 mg/mL
  • Ethanol 53 mg/mL
  • 存贮条件 储存温度-20°C

    描述

    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

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    注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途