| 產(chǎn)品描述： | Bivalirudin is a reversible inhibitor of α- and ζ-thrombin (Kis = 2.56 and 1.84 nM, respectively), enzymes that exhibit high fibrinogen-clotting activities. |
| 靶點(diǎn)： |
Thrombin |
| 體內(nèi)研究： |
Deposition in aspirin-treated groups receiving low-, medium-, and high-dose Bivalirudin decreased in a dose-dependent manner by 37%, 44%, and 56%, respectively. As the dose of Bivalirudin was increased, the plasma Bivalirudin levels and activated partial thromboplastin time ratios (final: initial) also increased in a dose-dependent manner. The mean plasma Bivalirudin levels ranged from 0.74 micrograms/ml in the low-dose Bivalirudin group to 2.55 micrograms/ml in the high-dose Bivalirudin group, and the corresponding activated partial thromboplastin time ratios were 1.5 and 3.3 |
| 動(dòng)物實(shí)驗(yàn)： |
Animals were randomly assigned to one of five groups: control (no aspirin or hirulog); aspirin alone (10 mg/kg); aspirin plus low-dose hirulog (0.2 mg/kg bolus followed by 0.5 mg/kg/hr); aspirin plus medium-dose hirulog (0.4 mg/kg bolus followed by 1.0 mg/kg/hr); or aspirin plus high-dose hirulog (0.6 mg/kg bolus followed by 1.5 mg/kg/hr). Hirulog was infused before surgery and continued until termination of the experiment 30 minutes after endarterectomy |
| 參考文獻(xiàn)： |
1.Hamelink JK, et al. Inhibition of platelet deposition by combined hirulog and aspirin in a rat carotid endarterectomy model. J Vasc Surg. 1995 Mar;21(3):492-8. 2.Witting JI, et al. Thrombin-specific inhibition by and slow cleavage of hirulog-1. Biochem J. 1992 May 1;283 ( Pt 3):737-43. 3.Ofosu FA, et al. Inhibition of the amplification reactions of blood coagulation by site-specific inhibitors of alpha-thrombin. Biochem J. 1992 May 1;283 ( Pt 3):893-7. |
| 溶解性： |
DMSO:10 mM |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
0.459 ml |
2.293 ml |
4.587 ml |
| 5 mM |
0.092 ml |
0.459 ml |
0.917 ml |
| 10 mM |
0.046 ml |
0.229 ml |
0.459 ml |
| 50 mM |
0.009 ml |
0.046 ml |
0.092 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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