Dabigatran (BIBR 953)

Catalog No.S2196

Dabigatran (BIBR 953) Chemical Structure

Molecular Weight(MW): 471.51

Dabigatran (BIBR 953) is a potent nonpeptide thrombin inhibitor with an IC50 of 9.3 nM in a cell-free assay.

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3 Customer Reviews

  • The peak fluorescence of each time course at the specified drug concentration are plotted as a function of concentration of (C) dabigatran. Each dose-response curve was fitted to the Hill equation, and these curves are shown in red for thrombin inhibitors (B,C).

    Sci Rep, 2016, 6:29387. Dabigatran (BIBR 953) purchased from Selleck.

    Thromb Res 2014 133 Suppl 1, S6-8. Dabigatran (BIBR 953) purchased from Selleck.

  • The effect of dabigatran on protease-activated receptor-1 thrombin receptor expression. Samples from healthy donors were spiked with dabigatran (0-10,000 ng/mL). The expression of thrombin receptor was tested with flow cytometry, n = 3. The SPAN12 antibody recognizes an epitope that is lost when thrombin cleaves the receptor, while WEDE15 antibody recognizes epitopes cleaved and uncleaved receptor. Results are means ± standard deviations. Comparisons were made with t test, *p < 0.05

    J Thromb Thrombolysis, 2017. Dabigatran (BIBR 953) purchased from Selleck.

Purity & Quality Control

Choose Selective Thrombin Inhibitors

Biological Activity

Description Dabigatran (BIBR 953) is a potent nonpeptide thrombin inhibitor with an IC50 of 9.3 nM in a cell-free assay.
Features Dabigatran is a reversible, competitive, direct thrombin inhibitor.
Targets
Thrombin [1]
(Cell-free assay)
9.3 nM
In vitro

BIBR 953 is a very potent anticoagulant. BIBR 953 shows that the terminal phenyl can be substituted by the more hydrophilic 2-pyridyl group without substantial loss of activity. BIBR 953 inhibits thrombin, plasmin, factor Xa, trypsin, tPA and activated protein C with Ki of 4.5 nM, 1.7 μM, 3.8 μM, 50 nM, 45 μM and 20 μM, respectively. [1] BIBR 953 specifically and reversibly inhibits thrombin. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 cells M4DGbmZ2dmO2aX;uJIF{e2G7 NHTmVlk{KG2rboO= MU\Jcohq[mm2aX;uJI9nKGi3bXHuJG9EXDJvbXXkbYF1\WRiQWPQL{B2eHSja3Wg[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDh[pRmeiB|IH3pcpMh[nliZnz1c5Jme2OnbnPlJIF{e2G7LDDJR|UxRTRwNzFOwG0> M2OyOVI{OjRzMEK5

... Click to View More Cell Line Experimental Data

In vivo BIBR 953 exhibits the most favorable activity profile following i.v. administration to rats. [1] The bioavailability of dabigatran after p.o. administration of dabigatran etexilate is 7.2%. Dabigatran is predominantly excreted in the feces after p.o. treatment and in the urine after i.v. treatment. The mean terminal half-life of dabigatran is approximately 8 hours. Dabigatran acylglucuronides accounts for 0.4% and 4% of the dose in urine after p.o. and i.v. dosing, respectively. [3]

Protocol

Solubility (25°C)

In vitro 10% Trifluoroacetic acid water solution 33 mg/mL (69.98 mM)
DMSO 0.5 mg/mL (1.06 mM)
Ethanol 0.01 mg/mL (0.02 mM)
In vivo Add solvents individually and in order:
10% Trifluoroacetic acid water solution
33 mg/mL

* 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 471.51
Formula

C25H25N7O3

CAS No. 211914-51-1
Storage powder
in solvent
Synonyms N/A

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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 --

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    We want to use this product for an in vivo study with rats, Do you have any suggestions?

  • Answer:

    Dabigatran (BIBR 593) has very low solubility in water or DMSO. We suggest that you dissolve dabigatran in aqueous acidic solution (The acids are preferably selected from among hydrochloric acid, hydrobromic acid, sulfuric acid, phosphoric acid, methansulphonic acid, acetic acid, fumaric acid, citric acid, tartaric acid, and maleic acid. Of particular interest is hydrochloric acid. ), with pH < 3, preferably < 2. Please refer to the following reference: http://www.sumobrain.com/patents/wipo/Lyophilised-dabigatran/WO2010086329.html.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID