替卡格雷

Ticagrelor (订货以英文为准)

编号:T125095
CAS号:274693-27-5
分子式:C23H28F2N6O4S
分子量:522.57
货号 品牌 包装 目录价 您的价格 库存 数量 购买
T125095-1g 阿拉丁 1g ¥129.90
T125095-100mg 阿拉丁 100mg ¥101.00
T125095-250mg 阿拉丁 250mg ¥49.90
T125095-25mg 阿拉丁 25mg ¥30.90
T125095-5g 阿拉丁 5g ¥449.90
T125095-500mg 阿拉丁 500mg ¥79.90
产品名称 Ticagrelor
中文名称 替卡格雷
CAS号 274693-27-5
分子式(M.F.) C23H28F2N6O4S
分子量(M.W.) 522.57
储存条件 避光;-20°C储存;充氩
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
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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