产品描述: | Dabigatran etexilate mesylate is the orally active prodrug of dabigatran. Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI, Ki: 4.5 nM). |
靶点: |
Thrombin |
体内研究: |
Dabigatran prolonged the aPTT dose-dependently after intravenous administration in rats (0.3, 1 and 3 mg/kg) and rhesus monkeys (0.15, 0.3 and 0.6 mg/kg). Dose- and time-dependent anticoagulant effects were observed with dabigatran etexilate administered orally to conscious rats (10, 20 and 50 mg/kg) or rhesus monkeys (1, 2.5 or 5 mg/kg), with maximum effects observed between 30 and 120 min after administration, respectively. Patients treated with dabigatran etexilate experienced fewer ischaemic strokes (3.74 dabigatran etexilate vs 3.97 warfarin) and fewer combined intracranial hemorrhages and hemorrhagic strokes (0.43 dabigatran etexilate vs 0.99 warfarin) per 100 patient-years |
参考文献: |
1.Kansal AR, Sorensen SV, Gani R, Cost-effectiveness of dabigatran etexilate for the prevention of stroke and systemic embolism in UK patients withatrial fibrillation. Heart. 2012 Apr;98(7):573-8. 2.Wienen W, Stassen JM, Priepke H, In-vitro profile and ex-vivo anticoagulant activity of the direct thrombin inhibitor dabigatran and its orally activeprodrug, dabigatran etexilate. Thromb Haemost. 2007 Jul;98(1):155-62. |
溶解性: |
Soluble in DMSO |
保存条件: |
2-8℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
1.382 ml |
6.908 ml |
13.815 ml |
5 mM |
0.276 ml |
1.382 ml |
2.763 ml |
10 mM |
0.138 ml |
0.691 ml |
1.382 ml |
50 mM |
0.028 ml |
0.138 ml |
0.276 ml |
|
注意: |
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