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Dabigatran

Catalog No. T6295 CAS 211914-51-1

Synonyms: BIBR 953ZW, 达比加群, BIBR 953

Dabigatran 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, CAS 211914-51-1

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Purity: 98%

Biological Description

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Storage & Solubility Information

Description	Dabigatran 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 953ZW, 达比加群, BIBR 953
Molecular Weight	471.521
Formula	C25H25N7O3
CAS No.	211914-51-1

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

0.1 M HCL: 12.5 mg/mL (26.51 mM), Need ultrasonic

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

H2O: < 0.1 mg/mL (insoluble)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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：

Coagulation and Anticoagulation Compound Library Drug-induced Liver Injury (DILI) Compound Library Anti-COVID-19 Compound Library

Related Products

Related compounds with same targets

Heparin sodium salt Dabigatran Enoxaparin sodium Argatroban Monohydrate Ximelagatran Odiparcil NFPS RWJ-445167

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Keywords

Dabigatran 211914-51-1 蛋白酶体 Thrombin Inhibitor BIBR-953 inhibit BIBR 953 BIBR 953ZW BIBR953 inhibitor

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