Dabigatran etexilate
Based on 4 publication(s) in Google Scholar
Dabigatran etexilate (BIBR 1048) is an orally active proagent of Dabigatran (a direct inhibitor of thrombin). Dabigatran etexilate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation.
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- Pureza : 99.92%
- No. CAS: 211915-06-9
- Fòrmula: C34H41N7O5
- Peso molecular:627.73
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Dabigatran etexilate
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Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Platelet | IC50 |
0.326 μM
Compound: Dabigatran etexilate
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Antiplatelet activity against rabbit platelets assessed as inhibition of thrombin-induced platelet aggregation
Antiplatelet activity against rabbit platelets assessed as inhibition of thrombin-induced platelet aggregation
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[PMID: 23043765] |
| Platelet | IC50 |
0.337 μM
Compound: Dabigatran etexilate
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Inhibition of thrombin-induced rabbit platelet aggregation compound pre-incubated in rabbit liver microsomal suspension
Inhibition of thrombin-induced rabbit platelet aggregation compound pre-incubated in rabbit liver microsomal suspension
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[PMID: 23466230] |
| Platelet | IC50 |
3.26 x 10-4 μM
Compound: Dabigatran
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Antiplatelet activity in New Zealand rabbit platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 1 min followed by thrombin addition measured after 10 mins
Antiplatelet activity in New Zealand rabbit platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 1 min followed by thrombin addition measured after 10 mins
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[PMID: 29432947] |
In Vivo
Dabigatran etexilate maximally and significantly prolongs partial thromboplastin time (aPTT) to 25.2, 38.4 and 78.3 s in 30 min after 10, 20 and 50 mg/kg oral doses, respectively[1].
Dabigatran etexilate maximally prolongs the aPTT to 34.3 s, 44.0 s, and 63.0 s, respectively, 2h after 1, 2.5 or 5 mg/kg doses in the monkey[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male rats (280-350 g) and rhesus monkeys of either sex (3-8 kg)[1]
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Dosage:10, 20 and 50 mg/kg for rats and 1, 2.5 and 5 mg/kg for monkeys
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Administration:Oral
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Result:Had dose- and time-dependent anticoagulant effects.
Chemical Information
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No. CAS 211915-06-9
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Appearance Solid
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Peso molecular 627.73
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Fòrmula C34H41N7O5
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Color White to off-white
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SMILES
O=C(N(C1=NC=CC=C1)CCC(OCC)=O)C2=CC=C3C(N=C(N3C)CNC4=CC=C(C(NC(OCCCCCC)=O)=N)C=C4)=C2
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Synonyms
BIBR 1048
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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J Nanobiotechnology
Multifunctional nanoagonist enhances photodynamic therapy-driven in situ cancer vaccination by inhibiting tumor thrombosis. [Abstract]2025 Nov 20;23(1):724. PMID: 41267013 -
Biochem Pharmacol
Dabigatran etexilate activation is affected by the CES1 genetic polymorphism G143E (rs71647871) and gender. [Abstract]2016 Nov 1:119:76-84. PMID: 27614009 -
J Chromatogr Sci
Characterization of the Fluorescent Spectra and Intensity of Dabigatran and Dabigatran Etexilate: Application to HPLC Analysis with Fluorescent Detection†. [Abstract]2016 Oct 17;54(9):1648-1651. PMID: 27473419 -
Elife
2022 Mar 23:11:e77444. PMID: 35294338
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (159.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.98 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.98 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (271 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Wienen W, et al. In-vitro profile and ex-vivo anticoagulant activity of the direct thrombin inhibitor dabigatran and its orally activeprodrug, dabigatran etexilate. Thromb Haemost. 2007 Jul;98(1):155-62. [Content Brief]
[2]. Blair HA, Keating GM. Dabigatran Etexilate: A Review in Nonvalvular Atrial Fibrillation. Drugs. 2017;77(3):331-344. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.5930 mL | 7.9652 mL | 15.9304 mL | 39.8260 mL |
| 5 mM | 0.3186 mL | 1.5930 mL | 3.1861 mL | 7.9652 mL | |
| 10 mM | 0.1593 mL | 0.7965 mL | 1.5930 mL | 3.9826 mL | |
| 15 mM | 0.1062 mL | 0.5310 mL | 1.0620 mL | 2.6551 mL | |
| 20 mM | 0.0797 mL | 0.3983 mL | 0.7965 mL | 1.9913 mL | |
| 25 mM | 0.0637 mL | 0.3186 mL | 0.6372 mL | 1.5930 mL | |
| 30 mM | 0.0531 mL | 0.2655 mL | 0.5310 mL | 1.3275 mL | |
| 40 mM | 0.0398 mL | 0.1991 mL | 0.3983 mL | 0.9957 mL | |
| 50 mM | 0.0319 mL | 0.1593 mL | 0.3186 mL | 0.7965 mL | |
| 60 mM | 0.0266 mL | 0.1328 mL | 0.2655 mL | 0.6638 mL | |
| 80 mM | 0.0199 mL | 0.0996 mL | 0.1991 mL | 0.4978 mL | |
| 100 mM | 0.0159 mL | 0.0797 mL | 0.1593 mL | 0.3983 mL |
Dabigatran etexilate Related Classifications
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