Dabigatran (ethyl ester) 

Dabigatran ethyl ester is an emerging oral anticoagulant which is a direct inhibitor of thrombin activity. IC50 value: Target: thrombin Dabigatran 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%.

499.56

C₂₇H₂₉N₇O₃

429658-95-7

Solid

White to off-white

O=C(N(C1=NC=CC=C1)CCC(OCC)=O)C2=CC=C3C(N=C(N3C)CNC4=CC=C(C(N)=N)C=C4)=C2

Room temperature in continental US; may vary elsewhere.

• [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