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产品名称 英文名称:Ticagrelor 同义词 Ticagrelor、274693-27-5、Brilinta、Brilique、AZD6140、Possia、AZD-6140、AR-C126532XX、AZD 6140、TICARGRELOR、UNII-GLH0314RVC、GLH0314RVC、CHEBI68558、(1S,2S,3R,5S)-3-(7-(((1R,2S)-2-(3,4-difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimid、替卡格雷、替格瑞洛、(1 S ,2 S ,3 R ,5 S )-3-7-{(1 R ,2 S )-2-(3,4-二氟苯基)环丙基 氨基 }-5-(丙基砜基)-3 H - 1,2,3 三唑 4,5- d 嘧啶-3-基-5-(2-羟乙氧基)-1,2-环戊二醇 产品性质 CAS编号:274693-27-5 分子式:C23H28F2N6O4S 分子量:522.57 PubChem编号:9871419 别名:替卡格雷|替格瑞洛|(1 S ,2 S ,3 R ,5 S )-3-7-{(1 R ,2 S )-2-(3,4-二氟苯基)环丙基 氨基 }-5-(丙基砜基)-3 H - 1,2,3 三唑 4,5- d 嘧啶-3-基-5-(2-羟乙氧基)-1,2-环戊二醇 英文别名:Ticagrelor|274693-27-5|Brilinta|Brilique|AZD6140|Possia|AZD-6140|AR-C126532XX|AZD 6140|TICARGRELOR|UNII-GLH0314RVC|GLH0314RVC|CHEBI68558|(1S,2S,3R,5S)-3-(7-(((1R,2S)-2-(3,4-difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimid 规格或纯度:≥98% 英文名称:Ticagrelor 生化机理:Ticagrelor is an active drμg 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 drμg available to bind platelets.Reversible antagonist of the platelet purinergic\xa0P2Y 12 receptor,\xa0the main receptor responsible for ADP- induced platelet aggregation. Changes the conformation of the P2Y 12 receptor, resulting in reversible, concentration dependent inhibition of th 储存温度:避光,-20°C储存,充氩 运输条件:超低温冰袋运输 备注:25mg卖完停产,不再备货 产品介绍:Ticagrelor (AZD6140) 是可逆的,可用来研究血小板聚集。Ticagrelor(AZD-6140) is the first reversibly binding oral P2Y12 receptor antagonist(Ki= 2 nM), also inhibits CYP2C9 and midazolam 4-hydroxylation with IC50 of 10.5 μM and 8.2 μM respectively.A reversible antagonist of the platelet purinergic P2Y12 receptor ALogP:2 IUPAC Name:(1S,2S,3R,5S)-3-[7-[[(1R,2S)-2-(3,4-difluorophenyl)cyclopropyl]amino]-5-propylsulfanyltriazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol INCHI:InChI=1S/C23H28F2N6O4S/c1-2-7-36-23-27-21(26-15-9-12(15)11-3-4-13(24)14(25)8-11)18-22(28-23)31(30-29-18)16-10-17(35-6-5-32)20(34)19(16)33/h3-4,8,12,15-17,19-20,32-34H,2,5-7,9-10H2,1H3,(H,26,27,28)/t12-,15+,16+,17-,19-,20+/m0/s1 InChi Key:OEKWJQXRCDYSHL-FNOIDJSQSA-N Canonical SMILES:CCCSC1=NC(=C2C(=N1)N(N=N2)C3CC(C(C3O)O)OCCO)NC4CC4C5=CC(=C(C=C5)F)F Isomeric SMILES:CCCSC1=NC(=C2C(=N1)N(N=N2)[C@@H]3C[C@@H]([C@H]([C@H]3O)O)OCCO)N[C@@H]4C[C@H]4C5=CC(=C(C=C5)F)F PubChem CID:9871419 ChEMBL Ligand:CHEMBL398435 Wikipedia:Ticagrelor CAS Registry No.:274693-27-5 ChEBI:CHEBI68558 RCSB PDB Ligand:TIQ PEP:ticagrelor Reactome Reaction:R-HSA-9611277 Reactome Drug:R-ALL-9611252 DrugCentral Ligand:4184 GPCRdb Ligand:ticagrelor 溶解性:DMSO 105 mg/mL Water <1 mg/mL Ethanol 53 mg/mL 敏感性:对光敏感 折光率:1.74 沸点:~777.6 °C at 760 mmHg 熔点:149-154°C 象形图: 信号词:Warning 危险声明:H315 Causes skin irritationH319 Causes serious eye irritationH335 May cause respiratory irritationH411 Toxic to aquatic life with long lasting effects 预防措施声明:P261,P305+P351+P338,P273,P280,P302+P352,P321,P405,P501,P264,P271,P304+P340,P403+P233,P362+P364,P391,P264+P265,P337+P317,P332+P317,P319 产品包装
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