| Size | Price | Stock | Qty |
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| 5mg |
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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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Purity: ≥98%
Dabigatran (formerly BIBR 953; Pradaxa; Prazaxa; BIBR 953ZW) is a potent, nonpeptide, reversible, selective and direct thrombin inhibitor used to treat blood clots. In a test without cells, it inhibits thrombin with an IC50 of 9.3 nM. Because of its highly polar, zwitterionic nature and poor oral absorption, dabigatran is intended to be transformed into an orally active prodrug, BIBR 1048. Thrombin is competitively inhibited by dabigatran. This inhibition happens quickly and can be reversed. Dabigatran inhibits thrombin, both free and clot-bound. Both in vitro and ex vivo anticoagulant efficacy of dabigatran has been shown.
| Targets |
thrombin (Ki = 4.5 nM)
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|---|---|
| ln Vitro |
Dabigatran (BIBR 953) doubles the activated partial thromboplastin time (aPTT), prothrombin time (PT), and ecarin clotting time (ECT) in human platelet-poor plasma at concentrations of 0.23, 0.83, and 0.18 μM, respectively. It also exhibits concentration-dependent anticoagulant effects in a variety of species in vitro[1].
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| ln Vivo |
Dabigatran (0.01-0.1 mg/kg; i.v.) inhibits the formation of clots with an ED50 of 0.033 mg/kg in Wessler model[3].
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| Animal Protocol |
Male rats (Wessler model)[3]
0.01, 0.03, 0.05 and 0.1 mg/kg Intravenous injection |
| References |
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| Molecular Formula |
C25H25N7O3
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|---|---|---|
| Molecular Weight |
471.51
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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 # |
211914-51-1
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| Related CAS # |
Dabigatran-d4 hydrochloride;Dabigatran-d3;1246817-44-6;Dabigatran etexilate;211915-06-9;Dabigatran etexilate mesylate;872728-81-9;Dabigatran (ethyl ester);429658-95-7;Dabigatran-d4;1618637-32-3;Dabigatran-13C6;1210608-88-0;Dabigatran-13C,d3
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| Appearance |
Solid powder
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| SMILES |
CN1C2=C(C=C(C=C2)C(=O)N(CCC(=O)O)C3=CC=CC=N3)N=C1CNC4=CC=C(C=C4)C(=N)N
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| InChi Key |
YBSJFWOBGCMAKL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H25N7O3/c1-31-20-10-7-17(25(35)32(13-11-23(33)34)21-4-2-3-12-28-21)14-19(20)30-22(31)15-29-18-8-5-16(6-9-18)24(26)27/h2-10,12,14,29H,11,13,15H2,1H3,(H3,26,27)(H,33,34)
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| Chemical Name |
3-[[2-[(4-carbamimidoylanilino)methyl]-1-methylbenzimidazole-5-carbonyl]-pyridin-2-ylamino]propanoic 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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|---|---|---|---|---|
| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1208 mL | 10.6042 mL | 21.2085 mL | |
| 5 mM | 0.4242 mL | 2.1208 mL | 4.2417 mL | |
| 10 mM | 0.2121 mL | 1.0604 mL | 2.1208 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 |
| NCT04045093 | Recruiting | Drug: Dabigatran etexilate Drug: Warfarin |
Atrial Fibrillation Mitral Stenosis |
The University of Hong Kong | October 22, 2020 | Phase 4 |
| NCT04695106 | Recruiting | Drug: Ticagrelor Drug: Dabigatran Etexilate |
Atrial Fibrillation Antithrombotic Therapy |
Medical University of Gdansk | October 25, 2021 | Phase 4 |
| NCT05491460 | Active Recruiting |
Drug: Apixaban 5 MG Tab Drug: Edoxaban 60Mg Tab |
Anticoagulant Therapy | Doasense GmbH | July 1, 2022 | Phase 1 |
| 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 |
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