Dabigatran (BIBR 953)
For research use only.
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.
Selleck's Dabigatran (BIBR 953) has been cited by 13 publications
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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
Choose Selective Thrombin Inhibitors
|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.|
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.  BIBR 953 specifically and reversibly inhibits thrombin. 
|In vivo||BIBR 953 exhibits the most favorable activity profile following i.v. administration to rats.  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. |
|In vitro||10% Trifluoroacetic acid water solution||33 mg/mL (69.98 mM)|
|DMSO||0.5 mg/mL (1.06 mM)|
* 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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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|
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.
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Frequently Asked Questions
We want to use this product for an in vivo study with rats, Do you have any suggestions?
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.