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Dabigatran

Catalog No. T6295   CAS 211914-51-1
Synonyms: BIBR 953, BIBR 953ZW

Dabigatran (BIBR 953ZW) is a THROMBIN inhibitor which acts by binding and blocking thrombogenic activity and the prevention of thrombus formation. It is used to reduce the risk of stroke and systemic EMBOLISM in patients with nonvalvular atrial fibrillation.

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Dabigatran Chemical Structure
Dabigatran, CAS 211914-51-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 36.00
2 mg In stock $ 52.00
5 mg In stock $ 85.00
10 mg In stock $ 143.00
25 mg In stock $ 283.00
50 mg In stock $ 477.00
100 mg In stock $ 698.00
500 mg In stock $ 1,470.00
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Purity: 98.65%
Purity: 97.44%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Dabigatran (BIBR 953ZW) is a THROMBIN inhibitor which acts by binding and blocking thrombogenic activity and the prevention of thrombus formation. It is used to reduce the risk of stroke and systemic EMBOLISM in patients with nonvalvular atrial fibrillation.
Targets&IC50 Thrombin: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]
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]
Synonyms BIBR 953, BIBR 953ZW
Molecular Weight 471.51
Formula C25H25N7O3
CAS No. 211914-51-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

0.1 M HCL: 12.5 mg/mL (26.51 mM), sonification is recommended.

DMSO: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 0.1 mg/mL (insoluble)

TargetMolReferences and Literature

1. Hauel NH, et al. J Med Chem. 2002, 45(9), 1757-1766. 2. Stangier J, et al. Br J Clin Pharmacol. 2007, 64(3), 292-303. 3. Blech S, et al. Drug Metab Dispos. 2008, 36(2), 386-399. 4. Alouidor B, Sweeney R E, Tat T, et al. Microfluidic Point-of-Care Ecarin-Based Clotting and Chromogenic Assays for Monitoring Direct Thrombin Inhibitors[J]. The journal of extra-corporeal technology. 2019, 51(1): 29-37.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Protease Inhibitor Library Bioactive Compounds Library Max Human Metabolite Library Drug-induced Liver Injury (DILI) Compound Library Pediatric Drug Library Clinical Compound Library Anti-Cardiovascular Disease Compound Library Coagulation and Anticoagulation Compound Library Anti-COVID-19 Compound Library

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Keywords

Dabigatran 211914-51-1 Proteases/Proteasome Thrombin Inhibitor BIBR 953 inhibit BIBR 953ZW BIBR953 BIBR-953 inhibitor

 

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