Dabigatran (BIBR-1048) etexilate

Catalog No.S2154

For research use only.

Dabigatran Etexilate (BIBR-1048) is the prodrug of dabigatran, a potent, nonpeptidic small molecule that specifically and reversibly inhibits both free and clot-bound thrombin by binding to the active site of the thrombin molecule.

Dabigatran (BIBR-1048) etexilate Chemical Structure

CAS No. 211915-06-9

Selleck's Dabigatran (BIBR-1048) etexilate has been cited by 8 Publications

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Biological Activity

Description Dabigatran Etexilate (BIBR-1048) is the prodrug of dabigatran, a potent, nonpeptidic small molecule that specifically and reversibly inhibits both free and clot-bound thrombin by binding to the active site of the thrombin molecule.
Targets
Thrombin [1]
In vitro

Dabigatran selectively and reversibly inhibits human thrombin (Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC50: 10 nM), while showing no inhibitory effect on other platelet-stimulating agents. Dabigatran selectively and reversibly inhibits human thrombin (Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC50: 10 nM), while showing no inhibitory effect on other platelet-stimulating agents. Dabigatran inhibits thrombin generation in platelet-poor plasma (PPP) with IC50 of 0.56 μM, measured as the endogenous thrombin potential (ETP). Dabigatran demonstrates concentrationdependent anticoagulant effects in various species in vitro, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) and ecarin clotting time (ECT) in human PPP at concentrations of 0.23, 0.83 and 0.18 μM, respectively. [1]

In vivo Dabigatran prolongs the aPTT dose-dependently after intravenous administration in rats (0.3, 1 and 3 mg/kg) and rhesus monkeys (0.15, 0.3 and 0.6 mg/kg). [1] Dabigatran etexilate (20 mg/kg, orally) produces less prolongation of K value and less decreases in angle and maximum amplitude than enoxaparin in swine. [2] Dabigatran (0.01-0.1 mg/kg) reduces thrombus formation dose-dependently, with an ED50 (50% of the effective dose) of 0.033 mg/kg and complete inhibition at 0.1 mg/kg. Dabigatran etexilate (5-30 mg/kg) inhibits thrombus formation in a dose- and time-dependent manner, with maximum inhibition within 30 min of pretreatment, suggesting a rapid onset of action.[3]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 126 mg/mL
(200.72 mM)
Water Insoluble
Ethanol '12 mg/mL

Chemical Information

Molecular Weight 627.73
Formula

C34H41N7O5

CAS No. 211915-06-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCCCCOC(=O)N=C(C1=CC=C(C=C1)NCC2=NC3=C(N2C)C=CC(=C3)C(=O)N(CCC(=O)OCC)C4=CC=CC=N4)N

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
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Molarity Calculator

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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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