Dabigatran

Catalog No.S2196 Batch:S219606

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Technical Data

Formula

C25H25N7O3
Molecular Weight 471.51 CAS No. 211914-51-1
Solubility (25°C)* In vitro DMSO Insoluble
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%5%TFA 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 0.300mg/ml (0.64mM) Taking the 1 mL working solution as an example, add 50 μL of 6 mg/ml clarified 5%TFA stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Dabigatran is a potent nonpeptide thrombin inhibitor with an IC50 of 9.3 nM in a cell-free assay.
Targets
Thrombin [1]
(Cell-free assay)
9.3 nM
In vitro BIBR 953 is a very potent anticoagulant. This compound shows that the terminal phenyl can be substituted by the more hydrophilic 2-pyridyl group without substantial loss of activity. It 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. This chemical specifically and reversibly inhibits thrombin.
In vivo BIBR 953 exhibits the most favorable activity profile following i.v. administration to rats. The bioavailability of this compound after p.o. administration of dabigatran etexilate is 7.2%. It is predominantly excreted in the feces after p.o. treatment and in the urine after i.v. treatment. The mean terminal half-life of this chemical is approximately 8 hours. Its acylglucuronides accounts for 0.4% and 4% of the dose in urine after p.o. and i.v. dosing, respectively.
Features Dabigatran is a reversible, competitive, direct thrombin inhibitor.

Protocol (from reference)

References

  • https://pubmed.ncbi.nlm.nih.gov/11960487/
  • https://pubmed.ncbi.nlm.nih.gov/17506785/
  • https://pubmed.ncbi.nlm.nih.gov/18006647/

Customer Product Validation

Data from [ Thromb Res , 2014 , 133 Suppl 1, S6-8 ]

<p>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</p>

, , J Thromb Thrombolysis, 2017, 44(2):216-222

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).

Data from [ , , Sci Rep, 2016, 6:29387 ]

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.

Data from [ , , Thromb Res, 2018, 170:97-101 ]

Selleck's Dabigatran Has Been Cited by 34 Publications

Effects of Heparin and Bivalirudin on Thrombin-Induced Platelet Activation: Differential Modulation of PAR Signaling Drives Divergent Prothrombotic Responses [ Frontiers in Cardiovascular Medicine, September 29, 2021, 717835] PubMed: 34660719
Hemorrhagic Transformation After Large Cerebral Infarction in Rats Pretreated With Dabigatran or Warfarin [ Stroke, October 2017, 2865-2871] PubMed: 37758192
Hemostasis stimulates lymphangiogenesis through release and activation of VEGFC [ Blood, November 14, 2019, 1764-1775] PubMed: 31562136
A rapid pro-hemostatic approach to overcome direct oral anticoagulants [ Nature Medicine, July 25, 2016, 924-932] PubMed: 27455511
An engineered factor Va prevents bleeding induced by direct-acting oral anticoagulants by different mechanisms [ Blood Advances, August 11, 2020, 3716-3727] PubMed: 32777068
HemoDens: A global hemostasis analyzer for kinetic characterization of clot formation, retraction, and lysis [ Thromb Res, 2025, 255:109480] PubMed: 40987075
Real-Time Imaging of Platelet-Initiated Plasma Clot Formation and Lysis Unveils Distinct Impacts of Anticoagulants [ Thromb Haemost, 2025, 10.1055/a-2497-4213] PubMed: 39788528
Dabigatran Attenuates the Binding of Thrombin to Platelets-A Novel Mechanism of Action [ Thromb Haemost, 2024, 10.1055/a-2483-0107] PubMed: 39586831
Detection of direct oral anticoagulants with the diluted Russel's viper venom time [ Int J Lab Hematol, 2024, 10.1111/ijlh.14300] PubMed: 38721750
DPP4 inhibition impairs senohemostasis to improve plaque stability in atherosclerotic mice [ J Clin Invest, 2023, 133(12)e165933] PubMed: 37097759

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.