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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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1g |
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Purity: ≥98%
Dabigatran Etexilate (BIBR-1048) is the prodrug of dabigatran used as an thrombin inhibitor to treat blood clot. It is a potent and nonpeptidic small molecule that binds to the active site of thrombin to specifically and reversibly inhibit thrombin both free and bound to clots. A powerful nonpeptide thrombin inhibitor, dabigatran (also called IBR 953) has an IC50 of 9.3 nM in a cell-free assay. Dabigatran's highly polar, zwitterionic nature and poor oral absorption make it intended to be transformed into an orally active prodrug, BIBR 1048. A competitive inhibition of thrombin is observed with dabigatran.
Targets |
Thrombin
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ln Vitro |
Dabigatran selectively and reversibly inhibits the thrombin-induced platelet aggregation (IC50: 10 nM) and human thrombin (Ki: 4.5 nM), but it has no inhibitory effect on other agents that stimulate platelets. Dabigatran selectively and reversibly inhibits the thrombin-induced platelet aggregation (IC50: 10 nM) and human thrombin (Ki: 4.5 nM), but it has no inhibitory effect on other agents that stimulate platelets. With an IC50 of 0.56 μM, dabigatran inhibits the production of thrombin in platelet-poor plasma (PPP), as determined by the endogenous thrombin potential (ETP). At 0.23, 0.83, and 0.18 μM, respectively, dabigatran doubles the activated partial thromboplastin time (aPTT), prothrombin time (PT), and ecarin clotting time (ECT) in human PPP. Dabigatran exhibits concentration-dependent anticoagulant effects in a variety of species in vitro.[1]
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ln Vivo |
Dabigatran extends the aPTT in rats (0.3, 1 and 3 mg/kg) and rhesus monkeys (0.15, 0.3 and 0.6 mg/kg) in a dose-dependent manner following intravenous administration. (Source: ) In comparison to enoxaparin, dabigatran etexilate (20 mg/kg) causes less prolongation of the K value, as well as less decreases in angle and maximum amplitude in swine. [/2] The dose-dependent reduction of thrombus formation by dabigatran (0.01-0.1 mg/kg) has an ED50 (50% of the effective dose) of 0.033 mg/kg and complete inhibition at 0.1 mg/kg. The dose- and time-dependent inhibition of thrombus formation by dabigatran etexilate (5-30 mg/kg) reaches its maximum within 30 minutes of pretreatment, indicating a quick onset of action. [/3]
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Animal Protocol |
Male rats (280-350 g) and rhesus monkeys of either sex (3-8 kg)
10, 20 and 50 mg/kg for rats and 1, 2.5 and 5 mg/kg for monkeys Oral |
References |
Molecular Formula |
C34H41N7O5
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Molecular Weight |
627.73
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Exact Mass |
627.32
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Elemental Analysis |
C, 65.05; H, 6.58; N, 15.62; O, 12.74)
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CAS # |
211915-06-9
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Appearance |
Solid powder
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SMILES |
CCCCCCOC(=O)NC(=N)C1=CC=C(C=C1)NCC2=NC3=C(N2C)C=CC(=C3)C(=O)N(CCC(=O)OCC)C4=CC=CC=N4.CS(=O)(=O)O
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InChi Key |
XETBXHPXHHOLOE-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C34H41N7O5.CH4O3S/c1-4-6-7-10-21-46-34(44)39-32(35)24-12-15-26(16-13-24)37-23-30-38-27-22-25(14-17-28(27)40(30)3)33(43)41(20-18-31(42)45-5-2)29-11-8-9-19-36-29;1-5(2,3)4/h8-9,11-17,19,22,37H,4-7,10,18,20-21,23H2,1-3H3,(H2,35,39,44);1H3,(H,2,3,4)
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Chemical Name |
ethyl 3-[[2-[[4-(N-hexoxycarbonylcarbamimidoyl)anilino]methyl]-1-methylbenzimidazole-5-carbonyl]-pyridin-2-ylamino]propanoate;methanesulfonic acid
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.5930 mL | 7.9652 mL | 15.9304 mL | |
5 mM | 0.3186 mL | 1.5930 mL | 3.1861 mL | |
10 mM | 0.1593 mL | 0.7965 mL | 1.5930 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT04695106 | Recruiting | Drug: Ticagrelor Drug: Dabigatran Etexilate |
Atrial Fibrillation Antithrombotic Therapy |
Medical University of Gdansk | October 25, 2021 | Phase 4 |
NCT03539055 | Active Recruiting |
Drug: Dabigatran Etexilate Oral Capsule |
Atrial Fibrillation Vanderbilt University Medical Center |
Vanderbilt University Medical Center |
September 1, 2018 | Phase 4 |
NCT04045093 | Recruiting | Drug: Dabigatran etexilate Drug: Warfarin |
Atrial Fibrillation Mitral Stenosis |
The University of Hong Kong | October 22, 2020 | Phase 4 |
NCT05536791 | Recruiting | Drug: Dabigatran Etexilate (DE) |
Venous Thromboembolism | Boehringer Ingelheim | November 24, 2022 | |
NCT05715658 | Recruiting | Drug: Dabigatran etexilate capsule |
Nonvalvular Atrial Fibrillation Health, Subjective |
Dongyang Liu | August 15, 2022 | Not Applicable |