产品说明书
Edoxaban
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同义名 : | 依杜沙班 ;DU-176;Savaysa;DU-176b |
| CAS号 : | 480449-70-5 | |
| 货号 : | A587736 | |
| 分子式 : | C24H30ClN7O4S | |
| 纯度 : | 98% | |
| 分子量 : | 548.058 | |
| MDL号 : | MFCD13195544 | |
| 存储条件： |
粉末 Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 9 mg/mL(16.42 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Factor Xa (FXa) is a coagulation factor thrombokinase responsible for the generation of thrombin. Edoxaban is a direct, selective FXa inhibitor with a Ki value of 0.561nM. In uman plasma samples, the minimum concentrations of edoxaban needed to significantly prolong prothrombin time (PT) and activated partial thromboplastin time were 55 and 50ng/mL, respectively. Plasma edoxaban at the concentration of 5.5 – 1640 ng/ml inhibited the generation of thrombin in a dose-dependent manner. Edoxaban above 10 ng/ml significantly extended the initiation phase of thrombin generation. In human platelet-poor plasma, the peak IC50 value, mRate IC50 value, and endogenous thrombin potential (ETP) IC50 value measured in thrombin generation assay were 0.145, 0.047, and 1.39 µM, respectively. The doses of edoxaban required to reach 50% of inhibition of CT2 lag time and ttPeak were 0.188 and 0.139 µM, respectively. In human platelet-rich plasma, the peak IC50, mRate IC50, and ETP IC50 values were 0.305, 0.230, and 0.636 µM, respectively. In apolipoprotein E (ApoE)-deficient mice, the treatment with 15 mg/kg edoxaban one hour before vascular injury almost completely prevented thrombus formation, and significantly decreased the time to occlusion and the patency rate. The following chronic oral administration of 10 mg/kg edoxaban by gavage b.i.d for six weeks significantly suppressed neointimal hyperplasia. | ||
| 作用机制 | Edoxaban inhibits free FXa by directly binding to FXa without the need of antithrombin, thereby preventing the conversion of prothrombin to thrombin. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00986154 | Venous Thromboembolism ... 展开 >> Deep Vein Thrombosis (DVT) Pulmonary Embolism (PE) Thromboembolism Venous Thrombosis 收起 << | Phase 3 | Completed | - | - |
| NCT02219984 | - | Active, not recruiting | July 2019 | Italy ... 展开 >> S. Orsola-Malpighi University hospital Bologna, BO, Italy, 40138 收起 << | |
| NCT02611635 | - | Completed | - | Sweden ... 展开 >> Multiple Locations, Sweden 收起 << | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.82mL 0.36mL 0.18mL |
9.12mL 1.82mL 0.91mL |
18.25mL 3.65mL 1.82mL |
| 参考文献 |
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