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Technical Data
| Formula | C34H41N7O5 |
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| Molecular Weight | 627.73 | CAS No. | 211915-06-9 | |
| Solubility (25°C)* | In vitro | DMSO | 126 mg/mL (200.72 mM) | |
| Ethanol | 12 mg/mL (19.11 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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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. | |
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| Targets |
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| 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)
References
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Customer Product Validation
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Data from [Thromb Res, 2014, 133 Suppl 1, S6-8]
Selleck's Dabigatran (BIBR-1048) etexilate has been cited by 8 publications
| Scanning laser-induced endothelial injury: a standardized and reproducible thrombosis model for intravital microscopy [ Sci Rep, 2022, 12(1):3955] | PubMed: 35273275 |
| The Malaria Parasite Plasmodium Falciparum in Red Blood Cells Selectively Takes Up Serum Proteins That Affect Host Pathogenicity [ Malar J, 2020, 15;19(1):155] | PubMed: 32295584 |
| Use of DOAC Stop for elimination of anticoagulants in the thrombin generation assay [Kopatz WF Thromb Res, 2018, 170:97-101] | PubMed: 30149286 |
| Modulatory Role of Nurr1 Activation and Thrombin Inhibition in the Neuroprotective Effects of Dabigatran Etexilate in Rotenone-Induced Parkinson's Disease in Rats. [ Mol Neurobiol, 2018, 55(5):4078-4089] | PubMed: 28585189 |
| In Vitro Selection of Specific DNA Aptamers Against the Anti-Coagulant Dabigatran Etexilate [Aljohani MM Sci Rep, 2018, 8(1):13290] | PubMed: 30185972 |
| Dabigatran reduces thrombin-induced platelet aggregation and activation in a dose-dependent manner. [Vinholt PJ, et al. J Thromb Thrombolysis, 2017, 44(2):216-222] | PubMed: 28580515 |
| A novel, rapid method to compare the therapeutic windows of oral anticoagulants using the Hill coefficient [Chang JB Sci Rep, 2016, 6:29387] | PubMed: 27439480 |
| A mouse bleeding model to study oral anticoagulants. [Monroe DM, et al. Thromb Res, 2014, 133 Suppl 1:S6-8] | PubMed: 24759147 |
RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.