Dabigatran Etexilate

Catalog No.S2154 Synonyms: BIBR-1048

Dabigatran Etexilate Chemical Structure

Molecular Weight(MW): 627.73

Dabigatran Etexilate is the prodrug of dabigatran, a potent, nonpeptidic small molecule that specifically and reversibly inhibits both free and clot-bound thrombin by binding to the active site of the thrombin molecule.

Size Price Stock Quantity  
In DMSO USD 430 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
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  • Thromb Res 2014 133 Suppl 1, S6-8. Dabigatran Etexilate purchased from Selleck.

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Biological Activity

Description Dabigatran Etexilate is the prodrug of dabigatran, a potent, nonpeptidic small molecule that specifically and reversibly inhibits both free and clot-bound thrombin by binding to the active site of the thrombin molecule.
Targets
Thrombin [1]
In vitro

Dabigatran selectively and reversibly inhibits human thrombin (Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC50: 10 nM), while showing no inhibitory effect on other platelet-stimulating agents. Dabigatran selectively and reversibly inhibits human thrombin (Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC50: 10 nM), while showing no inhibitory effect on other platelet-stimulating agents. Dabigatran inhibits thrombin generation in platelet-poor plasma (PPP) with IC50 of 0.56 μM, measured as the endogenous thrombin potential (ETP). Dabigatran demonstrates concentrationdependent anticoagulant effects in various species in vitro, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) and ecarin clotting time (ECT) in human PPP at concentrations of 0.23, 0.83 and 0.18 μM, respectively. [1]

In vivo Dabigatran prolongs the aPTT dose-dependently after intravenous administration in rats (0.3, 1 and 3 mg/kg) and rhesus monkeys (0.15, 0.3 and 0.6 mg/kg). [1] Dabigatran etexilate (20 mg/kg, orally) produces less prolongation of K value and less decreases in angle and maximum amplitude than enoxaparin in swine. [2] Dabigatran (0.01-0.1 mg/kg) reduces thrombus formation dose-dependently, with an ED50 (50% of the effective dose) of 0.033 mg/kg and complete inhibition at 0.1 mg/kg. Dabigatran etexilate (5-30 mg/kg) inhibits thrombus formation in a dose- and time-dependent manner, with maximum inhibition within 30 min of pretreatment, suggesting a rapid onset of action.[3]

Protocol

Solubility (25°C)

In vitro DMSO 126 mg/mL (200.72 mM)
Ethanol 12 mg/mL (19.11 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 627.73
Formula

C34H41N7O5

CAS No. 211915-06-9
Storage powder
Synonyms BIBR-1048

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02982850 Not yet recruiting Atrial Fibrillation|Valve Heart Disease Asan Medical Center|Boehringer Ingelheim December 2016 Phase 4
NCT02913326 Recruiting Thromboembolism Boehringer Ingelheim December 2016 Phase 3
NCT02744092 Recruiting Cancer|Venous Thromboembolism|Deep Vein Thrombosis (DVT)|Pulmonary Embolism (PE)|Blood Clot Alliance Foundation Trials, LLC.|Patient-Centered Outcomes Research Institute December 2016 --
NCT02945020 Recruiting Healthy Janssen Research & Development, LLC November 2016 Phase 1
NCT02979561 Recruiting Angiographically Confirmed Acute Massive Pulmonary Embolism Treated With Endovascular Mechanical Fragmentation and Thrombolytic Therapy Meshalkin Research Institute of Pathology of Circulation October 2016 Phase 4
NCT02631057 Completed Atrial Fibrillation Boehringer Ingelheim September 2016 --

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