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Ticagrelor 结构式

替卡格雷

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货号 :BCP05311CAS号 :274693-27-5纯度:98%
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  • 基本信息与产品描述
CAS号 274693-27-5 货号 BCP05311
中文名 替卡格雷
英文名 Ticagrelor
中文别名
英文别名 AR-C 126532XX;AZD 6140;AZD6140;AZD-6140; AR-C-126532XX; AR-C126532XX;
SMILES CCCSC1=NC2=C(C(=N1)NC3CC3C4=CC(=C(C=C4)F)F)N=NN2C5CC(C(C5O)O)OCCO
化学名称
分子式 C23H28F2N6O4S 分子量 522.57
纯度 98% 配送 惯例下常温包邮
产品描述 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. Ticagrelor moderately inhibits CYP2C9 activity in human liver microsomes, while exhibiting little or no inhibition of CYP1A2, CYP2B6, CYP2C8, CYP2C19, CYP2D6, and CYP2E1.
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