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Ticagrelor

替卡格雷,替格瑞洛,替格雷洛,AZD6140,AZD-6140,AZD 6140,AR-C 126532XX,

Ticagrelor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。

目录号
EY1357
EY1357
EY1357
EY1357
纯度
99.61%
99.61%
99.61%
99.61%
规格
1 mg
5 mg
10 mg
50 mg
原价
140
292
480
680
售价
140
292
480
680
库存
现货
现货
现货
现货
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  • 生物活性

    Ticagrelor is the first reversibly binding oral P2Y12 receptor antagonist with Ki of 2 nM.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] VAN Giezen JJ, et al. J Thromb Haemost, 2009, 7(9), 1556-1565.

    分子式
    C23H28F2N6O4S    		 分子量
    522.57    		 CAS号
    274693-27-5    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    105 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    55 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT02341729 Acute Coronary Syndrome Drug: ticagrelor University Hospital, Ghent|AstraZeneca Phase 4 2015-01-01 2015-01-16
    NCT02292277 Myocardial Infarction Drug: Ticagrelor Karolinska University Hospital|AstraZeneca 2014-10-01 2016-05-20
    NCT02335099 End Stage Renal Disease|Vascular Access Patency Drug: ticagrelor|Drug: Placebo University of Virginia|AstraZeneca Phase 1|Phase 2 2014-12-01 2016-10-24
    NCT02284048 Microvascular Angina Drug: ticagrelor Second Xiangya Hospital of Central South University Phase 4 2014-11-01 2014-11-05
    NCT02939248 Unstable Angina Pectoris Drug: Crushed ticagrelor followed by morphine|Drug: Crushed ticagrelor, morphine,naloxone Collegium Medicum w Bydgoszczy Phase 4 2016-10-01 2016-10-19
    NCT02939235 Unstable Angina Pectoris Drug: Crushed ticagrelor followed by morphine|Drug: Crushed ticagrelor, morphine,metoclopramide Collegium Medicum w Bydgoszczy Phase 4 2016-07-01 2016-12-20
    NCT02406911 Chronic Kidney Disease Drug: Ticagrelor Kyunghee University Medical Center Phase 3 2015-02-01 2015-03-30
    NCT02265068 Acute Coronary Syndrome (ACS) Drug: Ticagrelor IHF GmbH - Institut fr Herzinfarktforschung 2014-08-01 2017-02-17
    NCT02602444 Myocardial Infarction Drug: ticagrelor Collegium Medicum w Bydgoszczy 2015-10-01 2015-11-09
    NCT02612116 Unstable Angina Pectoris Drug: Pulverized ticagrelor sublingually|Drug: Pulverized ticagrelor orally|Drug: Integral ticagrelor Collegium Medicum w Bydgoszczy Phase 4 2015-09-01 2016-10-18
    NCT01876797 Healthy Drug: ticagrelor/prasugrel Asan Medical Center Phase 1 2013-07-01 2014-02-27
    NCT01962428 Non ST Segment Elevation Acute Coronary Syndrome Drug: ticagrelor General Hospital of Chinese Armed Police Forces Phase 4 2014-06-01 2016-09-21
    NCT01898442 Coronary Artery Disease Drug: Ticagrelor 180mg|Drug: Ticagrelor 270mg|Drug: Ticagrelor 360mg University of Florida Phase 2 2013-09-01 2015-05-26
    NCT01706510 Coronary Artery Disease Drug: Ticagrelor|Drug: Clopidogrel Rapid City Regional Hospital, Inc|AstraZeneca Phase 4 2012-12-01 2015-05-04
    NCT02518464 Migraine|Headache|Migraine Headache Drug: Ticagrelor 90 mg twice per day Columbia University|AstraZeneca Phase 4 2015-10-01 2016-04-21
    NCT02469740 Myocardial Ischemia|Coronary Artery Disease|Endothelial Dysfunction Drug: Ticagrelor|Drug: Clopidogrel University Hospital of Limerick Phase 4 2015-07-01 2016-03-10
    NCT02071966 Non ST Segment Elevation Acute Coronary Syndrome Drug: Ticagrelor|Drug: Clopidogrel Catholic University of the Sacred Heart Phase 4 2012-11-01 2016-07-25
    NCT03039205 Platelet Aggregation|Adenosine|Coronary Artery Disease|Kidney Dysfunction|Antiplatelet Therapy Drug: Clopidogrel|Drug: Ticagrelor University of Sao Paulo|Fundao de Amparo Pesquisa do Estado de So Paulo Phase 2 2017-02-15 2017-01-30
    NCT01226602 Blood Flow Speed|Coronary Flow Velocity Drug: AZD6140|Drug: Placebo AstraZeneca Phase 1 2010-12-01 2012-02-10
    NCT02064985 Stable Coronary Heart Disease (CHD) Drug: Inhibition of Platelet Aggregation by "Brilinta"(Ticagrelor) AstraZeneca Phase 4 2014-02-01 2016-04-05
    NCT02539160 Coronary Artery Disease|Diabetes Mellitus Drug: ticagrelor University of Florida Phase 4 2016-02-01 2017-03-15

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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