| 产品描述: | 产品介绍:Dabigatran etexilate mesylate (BIBR 1048MS) 是Dabigatran 前药。Dabigatran etexilate mesylate 具有抗凝作用,可以预防心房颤动引起的静脉血栓栓塞和中风。 Dabigatran etexilate mesylate (Pradaxa, BIBR 1048MS, Dabigatran etexilate methanesulfonate) 是Dabigatran是一种可逆的、选择性的、直接的 thrombin 凝血酶抑制剂(DTI)。Dabigatran 可选择性地、可逆地抑制人凝血酶,对应的Ki值为4.5 nM,和凝血酶诱导的血小板聚集,对应的IC50值为10 nM。; |
| 体内研究: |
Dabigatran etexilate mesylate (BIBR 1048MS; oral; 10, 20 and 50 mg/kg for rats and 1, 2.5 and 5 mg/kg for monkeys) has dose- and time-dependent anticoagulant effects and has maximum effects between 30 and 120 min after administration, respectively. Dabigatran etexilate mesylate maximally and significantly prolongs partial thromboplastin time (aPTT) to 25.2, 38.4 and 78.3 s in 30 min after 10, 20 and 50 mg/kg oral doses, respectively. Dabigatran etexilate mesylate maximally prolongs the aPTT to 34.3 s, 44.0 s, and 63.0 s, respectively, 2h after 1, 2.5 or 5 mg/kg doses in the monkey. |
| 参考文献: |
1. Wienen W, et al. 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. 2. Blair HA, Keating GM. Dabigatran Etexilate: A Review in Nonvalvular Atrial Fibrillation. Drugs. 2017;77(3):331-344. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.381 ml |
6.907 ml |
13.815 ml |
| 5 mM |
0.276 ml |
1.381 ml |
2.763 ml |
| 10 mM |
0.138 ml |
0.691 ml |
1.381 ml |
| 50 mM |
0.028 ml |
0.138 ml |
0.276 ml |
|
| 注意: |
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