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產品描述： Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM) |
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靶點：
Ki: 4.5 nM (thrombin);Thrombin |
體內研究：
Dabigatran (0.01-0.1 mg/kg; i.v.) inhibits clot formation with an ED50 of 0.033 mg/kg in Wessler model |
參考文獻：
1. 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. 2. Hauel NH, et al. Structure-based design of novel potent nonpeptide thrombin inhibitors. J Med Chem. 2002 Apr 25;45(9):1757-66. 3. Wienen W, et al. Effects of the direct thrombin inhibitor dabigatran and its orally active prodrug, dabigatran etexilate, on thrombus formation and bleeding time in rats. Thromb Haemost. 2007 Aug;98(2):333-8. |
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溶解性：
0.1 M HCL : 12.5 mg/mL (26.51 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble) DMSO : < 1 mg/mL (insoluble or slightly soluble) |
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保存條件：
-20℃ |
配置溶液濃度參考：
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1mg |
5mg |
10mg |
| 1 mM |
2.121 ml |
10.604 ml |
21.208 ml |
| 5 mM |
0.424 ml |
2.121 ml |
4.242 ml |
| 10 mM |
0.212 ml |
1.06 ml |
2.121 ml |
| 50 mM |
0.042 ml |
0.212 ml |
0.424 ml |
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| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
北京