ダビガトラン
Based on 7 publication(s) in Google Scholar
Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM).
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.06%
- CAS 番号: 211914-51-1
- 分子式: C25H25N7O3
- 分子量:471.51
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Dabigatran
More- Int J Biol Macromol. 2019 Aug 1:134:622-630. [Abstract]
- Biochem Pharmacol. 2016 Nov 1:119:76-84. [Abstract]
- ESC Heart Fail. 2026 May 5;13(3):xvag118. [Abstract]
- Platelets. 2021 Aug 18;32(6):807-814. [Abstract]
- Dig Dis Sci. 2019 Jan;64(1):102-112. [Abstract]
- LabMed. 2024 Nov 18.
- Elife. 2022 Mar 23:11:e77444. [Abstract]
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Others
生物活性
Ki: 4.5 nM (thrombin)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
25.3 μM
Compound: Dabigatran
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Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
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[PMID: 23241029] |
| HEK293 | IC50 |
4.7 μM
Compound: Dabigatran
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Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
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[PMID: 23241029] |
| HEK293 | IC50 |
8.1 μM
Compound: Dabigatran
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Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
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[PMID: 23241029] |
| Platelet | EC50 |
0.007 μM
Compound: Dabigatran
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Inhibition of thrombin induced platelet activation in CD-1 mouse plasma incubated for 2 mins by luminescence based assay
Inhibition of thrombin induced platelet activation in CD-1 mouse plasma incubated for 2 mins by luminescence based assay
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[PMID: 36462436] |
| Platelet | EC50 |
0.029 μM
Compound: Dabigatran
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Inhibition of tissue factor induced platelet activation in 76% human blood incubated for 15 mins by CD62 antibody based assay
Inhibition of tissue factor induced platelet activation in 76% human blood incubated for 15 mins by CD62 antibody based assay
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[PMID: 36462436] |
| Platelet | IC50 |
0.6 μM
Compound: Dabigatran
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Anticoagulant activity in mouse plasma assessed inhibition of thrombin-induced platelet aggregation
Anticoagulant activity in mouse plasma assessed inhibition of thrombin-induced platelet aggregation
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[PMID: 34902735] |
Dabigatran (BIBR 953) shows concentration-dependent anticoagulant effects in various species in vitro, doubling 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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male rats (Wessler model)[3]
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Dosage:0.01, 0.03, 0.05 and 0.1 mg/kg
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Administration:Intravenous injection
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Result:Inhibited clot formation with an ED50 of 0.033 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 211914-51-1
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性状 Solid
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分子量 471.51
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分子式 C25H25N7O3
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Color White to light yellow
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SMILES
N=C(N)C(C=C1)=CC=C1NCC2=NC3=CC(C(N(CCC(O)=O)C4=NC=CC=C4)=O)=CC=C3N2C
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別名
Dabigatran; BIBR 953; BIBR 953ZW
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Int J Biol Macromol
Natural constituents of St. John's Wort inhibit the proteolytic activity of human thrombin. [Abstract]2019 Aug 1:134:622-630. PMID: 31047931 -
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 -
ESC Heart Fail
Inhibition of adenosine kinase alleviates hypertrophic cardiomyopathy by ameliorating coronary microvascular dysfunction. [Abstract]2026 May 5;13(3):xvag118. PMID: 42015547 -
Platelets
Factor Xa and thrombin induce endothelial progenitor cell activation. The effect of direct oral anticoagulants. [Abstract]2021 Aug 18;32(6):807-814. PMID: 32762584 -
Dig Dis Sci
2019 Jan;64(1):102-112. PMID: 30288660 -
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Elife
2022 Mar 23:11:e77444. PMID: 35294338
Dabigatran purchased from MedChemExpress. Usage Cited in: Elife. 2022 Mar 23:11:e77444. [Abstract]
Vero cells with rVSVG/SARS-CoV-2 pseudovirus pretreated for 4 hr with 10 µM Camostat, Nafamostat, Dabigatran, or Otamixaban, compared with uninfected or infected/untreated cells.
溶剤 & 溶解度
0.1 M HCl : 12.5 mg/mL (26.51 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
DMSO : < 1 mg/mL (insoluble or slightly soluble)
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (272 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Wienen W, Stassen JM, Priepke H, 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]. Hauel NH, et al. Structure-based design of novel potent nonpeptide thrombin inhibitors. J Med Chem. 2002 Apr 25;45(9):1757-66. [Content Brief]
[3]. Wienen W, et al. Effects of the direct thrombin inhibitor dabigatran and its orally active prodrug, dabigatran etexilate, on thrombus formation and bleeding time in rats. Thromb Haemost. 2007 Aug;98(2):333-8. [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 |
|---|---|---|---|---|---|
| 0.1 M HCl | 1 mM | 2.1208 mL | 10.6042 mL | 21.2085 mL | 53.0211 mL |
| 5 mM | 0.4242 mL | 2.1208 mL | 4.2417 mL | 10.6042 mL | |
| 10 mM | 0.2121 mL | 1.0604 mL | 2.1208 mL | 5.3021 mL | |
| 15 mM | 0.1414 mL | 0.7069 mL | 1.4139 mL | 3.5347 mL | |
| 20 mM | 0.1060 mL | 0.5302 mL | 1.0604 mL | 2.6511 mL | |
| 25 mM | 0.0848 mL | 0.4242 mL | 0.8483 mL | 2.1208 mL |
Dabigatran 関連分類
HY-10163 関連分類
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