Dabigatran (BIBR 953)

For research use only.

Catalog No.S2196

13 publications

Dabigatran (BIBR 953) Chemical Structure

CAS No. 211914-51-1

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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Selleck's Dabigatran (BIBR 953) has been cited by 13 publications

4 Customer Reviews

  • 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, 44(2):216-222. Dabigatran (BIBR 953) purchased from Selleck.

  • 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.

  • Z-GLy-Gly-Arg-AMC cleavage by the calibrator in the absence or presence of dabigatran, influence of treatment with DOAC Stop. NPP was spiked with increasing concentrations of dabigatran and divided in two portions. One portion was left unaltered, while the other portion was treated with DOAC Stop (1 mL per tablet). Prepared samples were used to generate calibration curves according to normal CAT operation procedures.

    Thromb Res, 2018, 170:97-101. Dabigatran (BIBR 953) purchased from Selleck.

Purity & Quality Control

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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.
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 NH7OWYZHfW6ldHnvckBie3OjeR?= NFO3NVM{KG2rboO= M{DLOGlvcGmkaYTpc44hd2ZiaIXtZY4hV0OWMj3t[YRq[XSnZDDBV3AsKHWydHHr[UBmgHC{ZYPz[YQhcW5iSFXLNlk{KGOnbHzzJIFnfGW{IEOgcYlveyCkeTDmcJVwemW|Y3XuZ4Uh[XO|YYmsJGlEPTB;ND63JO69VQ>? NEHscm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{K0NVAzQSd-MkOyOFExOjl:L3G+
KB-3-1 MWnxTHRUKGG|c3H5 NUGxVmtDWC2pbInjc5Bzd3SnaX6gd5Vje3S{YYTld{Bq\GWwdHnmbYVlKGmwIFvCMVMuOSCjZHXuc4NiemOrbn;tZUBk\WyuIHzpcoUtKHGKVGOgeIhmemGyZYX0bYMhdGmkcnHyfUB{[3KnZX6= M4LLZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkSxNFI6Lz5{M{K0NVAzQTxxYU6=
HEK293 MXXGeY5kfGmxbjDhd5NigQ>? MWSxMlUhdWmwcx?= NIjvT5JKdmirYnn0bY9vKG:oIHj1cYFvKE2DVFWyT{1u\WSrYYTl[EBCW1BtIIXweIFs\SCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIx{KGGodHXyJFEvPSCvaX7zJIJ6KG[udX;y[ZNk\W6lZTDhd5NigSxiSVO1NF0zPS5|zszN M2rpc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkSxNFI6Lz5{M{K0NVAzQTxxYU6=

... 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]


Solubility (25°C)

In vitro 10% Trifluoroacetic acid water solution 33 mg/mL (69.98 mM)
DMSO 0.5 mg/mL (1.06 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 471.51


CAS No. 211914-51-1
Storage powder
in solvent
Synonyms N/A
Smiles CN1C2=C(C=C(C=C2)C(=O)N(CCC(=O)O)C3=CC=CC=N3)N=C1CNC4=CC=C(C=C4)C(=N)N

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04782076 Recruiting Drug: Dabigatran|Drug: Selpercatinib Healthy Loxo Oncology Inc.|Eli Lilly and Company March 5 2021 Phase 1
NCT04459585 Completed Drug: Dabigatran Etexilate Mesylate|Drug: Quizartinib Healthy Subjects|Drug-drug Interaction|Pharmacokinetics|Quizartinib Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. September 17 2020 Early Phase 1
NCT04532528 Recruiting Drug: Dabigatran Atrial Fibrillation Boehringer Ingelheim August 27 2020 --
NCT04433481 Recruiting Drug: Dabigatran|Other: Placebo Liver Cirrhosis|Portal Vein Thrombosis Institute of Liver and Biliary Sciences India June 20 2020 Not Applicable

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