Home Proteases Thrombin inhibitor Dabigatran (BIBR-1048) etexilate For research use only.

Dabigatran (BIBR-1048) etexilate

Synonyms: BIBR-1048

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

Dabigatran (BIBR-1048) etexilate Chemical Structure

CAS No. 211915-06-9

Purity & Quality Control

Dabigatran (BIBR-1048) etexilate Related Products

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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06360055 Recruiting
Health
Peking University Third Hospital
 April 1 2024 Not Applicable
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

Chemical Information & Solubility

Molecular Weight 627.73 Formula

C34H41N7O5
CAS No. 211915-06-9 SDF Download Dabigatran (BIBR-1048) etexilate SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 126 mg/mL ( (200.72 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 12 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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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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