Home Proteases Thrombin inhibitor Dabigatran For research use only.

Dabigatran

Synonyms: BIBR 953

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

Dabigatran Chemical Structure

Dabigatran Chemical Structure

CAS: 211914-51-1

Selleck's Dabigatran has been cited by 22 Publications

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Purity & Quality Control

Batch: Purity: 99.91%
99.91

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 cells Function assay 3 mins Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay, IC50=4.7 μM 23241029
KB-3-1 qHTS assay P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen 23241029
HEK293 Function assay 1.5 mins Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay, IC50=25.3μM 23241029
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Biological Activity

Description Dabigatran 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
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]
In Vivo
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05966740 Recruiting Venous Thromboembolism Boehringer Ingelheim|Children''s Hospital Acquired Thrombosis consortium October 31 2023 --
NCT05673889 Completed Healthy Pfizer|Arvinas Estrogen Receptor Inc. January 27 2023 Phase 1
NCT05715658 Recruiting Nonvalvular Atrial Fibrillation|Health Subjective Dongyang Liu|Peking University Third Hospital August 15 2022 Not Applicable
NCT05471817 Completed Vasomotor Symptoms as a Sex Hormone-dependent Disorder in Women and Men|Hot Flashes|Healthy Volunteers Bayer August 5 2022 Phase 1

Chemical lnformation & Solubility

Molecular Weight 471.51 Formula

C25H25N7O3
CAS No. 211914-51-1 SDF Download Dabigatran SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 0.5 mg/mL ( (1.06 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 0.01 mg/mL

Water : Insoluble


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In vivo
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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 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.

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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