Dabigatran (BIBR 953)

Catalog No.S2196

For research use only.

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

Dabigatran (BIBR 953) Chemical Structure

CAS No. 211914-51-1

Selleck's Dabigatran (BIBR 953) has been cited by 18 publications

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.
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 M4THO2Z2dmO2aX;uJIF{e2G7 M4TrNVMhdWmwcx?= NVLveHFSUW6qaXLpeIlwdiCxZjDoeY1idiCRQ2SyMY1m\GmjdHXkJGFUWCtidYD0ZYtmKGW6cILld5Nm\CCrbjDISWszQTNiY3XscJMh[W[2ZYKgN{BucW6|IHL5JIZtfW:{ZYPj[Y5k\SCjc4PhfUwhUUN3ME20Mlch|ryP M{L6V|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkSxNFI6Lz5{M{K0NVAzQTxxYU6=
KB-3-1 MmK2dWhVWyCjc4PhfS=> MlflVE1odHmlb4Dyc5RmcW5ic4Xid5Rz[XSnczDp[IVvfGmoaXXkJIlvKEuELUOtNUBi\GWwb3PhdoNqdm:vYTDj[YxtKGyrbnWsJJFJXFNidHjldoFx\XW2aXOgcIljemG{eTDzZ5Jm\W5? NXjSXm0yRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyOFExOjlpPkKzNlQyODJ7PD;hQi=>
HEK293 NXXSO4R7TnWwY4Tpc44h[XO|YYm= M4\XVFEvPSCvaX7z MVTJcohq[mm2aX;uJI9nKGi3bXHuJG1CXEV{Sz3t[YRq[XSnZDDBV3AsKHWydHHr[UBmgHC{ZYPz[YQhcW5iSFXLNlk{KGOnbHzzJIFnfGW{IEGuOUBucW6|IHL5JIZtfW:{ZYPj[Y5k\SCjc4PhfUwhUUN3ME2yOU4{|ryP MnvPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{NEGwNlkoRjJ|MkSxNFI6RC:jPh?=
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 (from reference)

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

Chemical Information

Molecular Weight 471.51
Formula

C25H25N7O3

CAS No. 211914-51-1
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05073627 Not yet recruiting Drug: Dicloxacillin Healthy Volunteers|Drug-drug Interaction University of Southern Denmark February 1 2022 Phase 1
NCT04942873 Not yet recruiting Other: adherence Nonvalvular Atrial Fibrillation Second Affiliated Hospital School of Medicine Zhejiang University July 20 2021 --
NCT05068414 Recruiting Diagnostic Test: Blood panel Atrial Fibrillation|Acute Coronary Syndrome|Thrombosis|Hemorrhage Centre Hospitalier Universitaire de Nīmes April 12 2021 --
NCT04782076 Completed Drug: Dabigatran|Drug: Selpercatinib Healthy Loxo Oncology Inc.|Eli Lilly and Company March 5 2021 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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