Home Proteases Thrombin inhibitor Dabigatran etexilate mesylate For research use only.

Dabigatran etexilate mesylate

Synonyms: Pradaxa, BIBR 1048MS, Dabigatran etexilate methanesulfonate

Dabigatran etexilate mesylate (Pradaxa, BIBR 1048MS, Dabigatran etexilate methanesulfonate) is an orally active prodrug of Dabigatran which is a reversible and selective, direct thrombin inhibitor (DTI). Dabigatran selectively and reversibly inhibits human thrombin with Ki of 4.5 nM and thrombin-induced platelet aggregation with IC50 of 10 nM.

Dabigatran etexilate mesylate Chemical Structure

Dabigatran etexilate mesylate Chemical Structure

CAS: 872728-81-9

Selleck's Dabigatran etexilate mesylate has been cited by 1 publication

Purity & Quality Control

Batch: S596001 DMSO] 100 mg/mL] false] Ethanol] 20 mg/mL] false] Water] Insoluble] false Purity: 99.94%
99.94

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Biological Activity

Description Dabigatran etexilate mesylate (Pradaxa, BIBR 1048MS, Dabigatran etexilate methanesulfonate) is an orally active prodrug of Dabigatran which is a reversible and selective, direct thrombin inhibitor (DTI). Dabigatran selectively and reversibly inhibits human thrombin with Ki of 4.5 nM and thrombin-induced platelet aggregation with IC50 of 10 nM.
Targets
human thrombin [1]
(Cell-free assay)
4.5 nM(Ki)
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02839746 Completed Atrial Fibrillation Boehringer Ingelheim June 13 2016 --
NCT02684981 Completed Atrial Fibrillation|Stroke Boehringer Ingelheim November 11 2015 --
NCT02433366 Completed Atrial Fibrillation Boehringer Ingelheim January 2015 --
NCT01139658 Completed Venous Thromboembolism Boehringer Ingelheim August 2010 --

Chemical lnformation & Solubility

Molecular Weight 723.84 Formula

C35H45N7O8S
CAS No. 872728-81-9 SDF --
Smiles CCCCCCOC(=O)NC(=N)C1=CC=C(NCC2=NC3=C(C=CC(=C3)C(=O)N(CCC(=O)OCC)C4=CC=CC=N4)[N]2C)C=C1.C[S](O)(=O)=O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (138.15 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 20 mg/mL

Water : Insoluble


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In vivo
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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.

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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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