Dabigatran ethyl ester

达比加群乙酯是一种新兴的口服抗凝剂，是凝血酶活性的直接抑制剂。

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库存: 现货

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5mg

￥650.00

520.00

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10mg

￥1087.00

870.00

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50mg

￥3425.00

2740.00

- +
100mg

￥5725.00

4580.00

- +

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Background

Dabigatran ethyl ester is an emerging oral anticoagulant which is a direct inhibitor of thrombin activity. IC50 value:Target: thrombinDabigatran provides a stable anticoagulation effect without any need to perform periodical laboratory controls. Of note, there is a growing amount of clinical evidence which shows its safety and efficacy. For these reasons, Dabigatran may suppose a revolution in oral anticoagulation. Dabigatran etexilate was rapidly converted to Dabigatran, with peak plasma dabigatran concentrations being attained after approximately 1.5 h; the bioavailability of Dabigatran after p.o. administration of Dabigatran etexilate was 7.2%.

参考文献:
[1]. Simon Michaelis, Anett Marais, Anna K. Schrey, et al. Dabigatran and Dabigatran Ethyl Ester: Potent Inhibitors of Ribosyldihydronicotinamide Dehydrogenase (NQO2). J. Med. Chem., 2012, 55 (8):3934-3944
[2]. Preetpal Singh Sidhu,Aiye Liang, Akul Y. Mehta,et al. Rational Design of Potent, Small, Synthetic Allosteric Inhibitors of Thrombin. J Med Chem. 2011; 54(15): 5522-5531.
[3]. Santiago Redondo, Maria-Paz Martínez, Marta Ramajo, et al. Pharmacological basis and clinical evidence of dabigatran therapy. J Hematol Oncol. 2011; 4: 53.
[4]. Stefan Blech, Thomas Ebner, Eva Ludwig-Schwellinger,et al. The Metabolism and Disposition of the Oral Direct Thrombin Inhibitor, Dabigatran, in Humans. DMD ,2008 , 36 (2) 386-399
[5]. Dabigatran

Protocol

Kinase experiment:

NQO2 (0.5 μM) is incubated with the substrate mitomycin C (50 μM) and four different Dabigatran concentrations in 100 mM potassium phosphate buffer (pH 5.8) at room temperature for 5 min prior to the addition of NADH (in increasing concentrations) as a cosubstrate and photometric monitoring at 340 nm for 30 min at rt. Ki values are determined. Data generated are used to calculate the IC50 of inhibition of NQO2 activity[1].

参考文献:

[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.