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Technical Data
| Formula | C25H25N7O3 |
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| Molecular Weight | 471.51 | CAS No. | 211914-51-1 | |
| Solubility (25°C)* | In vitro | 5%TFA | 6.09 mg/mL (12.91 mM) | |
| DMSO | Insoluble | |||
| 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 is a potent nonpeptide thrombin inhibitor with an IC50 of 9.3 nM in a cell-free assay. | ||
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| Targets |
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| 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] | ||
| Features | Dabigatran is a reversible, competitive, direct thrombin inhibitor. |
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]
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, , J Thromb Thrombolysis, 2017, 44(2):216-222
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Data from [Data independently produced by , , Sci Rep, 2016, 6:29387]
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Data from [Data independently produced by , , Thromb Res, 2018, 170:97-101]
Selleck's Dabigatran has been cited by 23 publications
| DPP4 inhibition impairs senohemostasis to improve plaque stability in atherosclerotic mice [ J Clin Invest, 2023, 133(12)e165933] | PubMed: 37097759 |
| OKL-1111, A modified cyclodextrin as a potential universal reversal agent for anticoagulants [ Thromb Res, 2023, 227:17-24] | PubMed: 37207560 |
| Thrombin induces ACSL4-dependent ferroptosis during cerebral ischemia/reperfusion [ Signal Transduct Target Ther, 2022, 7(1):59] | PubMed: 35197442 |
| Scanning laser-induced endothelial injury: a standardized and reproducible thrombosis model for intravital microscopy [ Sci Rep, 2022, 12(1):3955] | PubMed: 35273275 |
| Aortic intimal resident macrophages are essential for maintenance of the non-thrombogenic intravascular state [ Nat Cardiovasc Res, 2022, 1(1):67-84] | PubMed: 35599984 |
| Induced forms of α2-macroglobulin neutralize heparin and direct oral anticoagulant effects [ Int J Biol Macromol, 2021, 184:209-217] | PubMed: 34126147 |
| Unveiling the complex effects of direct oral anticoagulants on dilute Russell's viper venom time assays [ J Thromb Haemost, 2020, 18(8):1866-1873] | PubMed: 32294291 |
| Unveiling the complex effects of direct oral anticoagulants on dilute Russell's viper venom time assays [ Journal of Thrombosis and Haemostasis, 2020, 1866-1873] | PubMed: None |
| An engineered factor Va prevents bleeding induced by direct-acting oral anticoagulants by different mechanisms [ Blood Adv, 2020, 4(15):3716-3727] | PubMed: 32777068 |
| Whole Blood Point-of-Care Testing for Incomplete Reversal With Idarucizumab in Supratherapeutic Dabigatran. [ Anesth Analg, 2020, 130(2):535-541] | PubMed: 31490820 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
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.