Dabigatran ethyl ester hydrochloride |
| Catalog No.GC35802 |
Le chlorhydrate de dabigatran ester éthylique est un puissant inhibiteur de la ribosyldihydronicotinamide déshydrogénase (NQO2) avec une valeur IC50 de 0,8 μM et un inhibiteur de la thrombine.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 211914-50-0
Sample solution is provided at 25 µL, 10mM.
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Dabigatran ethyl ester hydrochloride is a potent inhibitor of ribosyldihydronicotinamide dehydrogenase (NQO2) with an IC50 value of 0.8 μM and a thrombin inhibitor. IC50: 0.8 μM (NQO2)[1]
The Ki of dabigatran (ethyl ester hydrochloride) toward NQO2 is 0.9 μM and the IC50 is 0.8 μM. The ethyl ester group of dabigatran (ethyl ester hydrochloride) significantly extends the interaction surface especially with hydrophobic amino acids such as Ile 128 and Met 154. Dabigatran ethyl ester has higher affinity than Dabigatran to both thrombin and NQO2[1]. Dabigatran is a highly selective, reversible, and potent thrombin inhibitor and is orally available as the prodrug, dabigatran etexilate[2].
Dabigatran (Ki=4.5 nM) could bind to human thrombin selectively, and reversibly to realize a strong and long-lasting anticoagulant effect[3].
[1]. Michaelis S, et al. Dabigatran and dabigatran ethyl ester: potent inhibitors of ribosyldihydronicotinamide dehydrogenase (NQO2). J Med Chem. 2012 Apr 26;55(8):3934-44. [2]. Eisert WG, et al. Dabigatran: an oral novel potent reversible nonpeptide inhibitor of thrombin. Arterioscler Thromb Vasc Biol. 2010 Oct;30(10):1885-9. [3]. Hauel NH, et al. Structure-based design of novel potent nonpeptide thrombin inhibitors. J Med Chem. 2002 Apr 25;45(9):1757-66.
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