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Synonyms | BIBR-1048 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C34H41N7O5 |
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分子量 | 627.73 | CAS No. | 211915-06-9 | |
Solubility (25°C)* | 体外 | DMSO | 126 mg/mL (200.72 mM) | |
Ethanol | 12 mg/mL (19.11 mM) | |||
Water | Insoluble | |||
* <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. |
製品説明 | Dabigatran Etexilate (BIBR-1048) is the prodrug of dabigatran, a potent, nonpeptidic small molecule that specifically and reversibly inhibits both free and clot-bound thrombin by binding to the active site of the thrombin molecule. |
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in vitro | Dabigatran selectively and reversibly inhibits human thrombin (Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC50: 10 nM), while showing no inhibitory effect on other platelet-stimulating agents. Dabigatran selectively and reversibly inhibits human thrombin (Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC50: 10 nM), while showing no inhibitory effect on other platelet-stimulating agents. Dabigatran inhibits thrombin generation in platelet-poor plasma (PPP) with IC50 of 0.56 μM, measured as the endogenous thrombin potential (ETP). Dabigatran demonstrates concentrationdependent anticoagulant effects in various species in vitro, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) and ecarin clotting time (ECT) in human PPP at concentrations of 0.23, 0.83 and 0.18 μM, respectively. [1] |
in vivo | Dabigatran prolongs the aPTT dose-dependently after intravenous administration in rats (0.3, 1 and 3 mg/kg) and rhesus monkeys (0.15, 0.3 and 0.6 mg/kg). [1] Dabigatran etexilate (20 mg/kg, orally) produces less prolongation of K value and less decreases in angle and maximum amplitude than enoxaparin in swine. [2] Dabigatran (0.01-0.1 mg/kg) reduces thrombus formation dose-dependently, with an ED50 (50% of the effective dose) of 0.033 mg/kg and complete inhibition at 0.1 mg/kg. Dabigatran etexilate (5-30 mg/kg) inhibits thrombus formation in a dose- and time-dependent manner, with maximum inhibition within 30 min of pretreatment, suggesting a rapid onset of action.[3] |
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Data from [Thromb Res, 2014, 133 Suppl 1, S6-8]
Scanning laser-induced endothelial injury: a standardized and reproducible thrombosis model for intravital microscopy [ Sci Rep, 2022, 12(1):3955] | PubMed: 35273275 |
The Malaria Parasite Plasmodium Falciparum in Red Blood Cells Selectively Takes Up Serum Proteins That Affect Host Pathogenicity [ Malar J, 2020, 15;19(1):155] | PubMed: 32295584 |
Use of DOAC Stop for elimination of anticoagulants in the thrombin generation assay [Kopatz WF Thromb Res, 2018, 170:97-101] | PubMed: 30149286 |
Modulatory Role of Nurr1 Activation and Thrombin Inhibition in the Neuroprotective Effects of Dabigatran Etexilate in Rotenone-Induced Parkinson's Disease in Rats. [ Mol Neurobiol, 2018, 55(5):4078-4089] | PubMed: 28585189 |
In Vitro Selection of Specific DNA Aptamers Against the Anti-Coagulant Dabigatran Etexilate [Aljohani MM Sci Rep, 2018, 8(1):13290] | PubMed: 30185972 |
Dabigatran reduces thrombin-induced platelet aggregation and activation in a dose-dependent manner. [Vinholt PJ, et al. J Thromb Thrombolysis, 2017, 44(2):216-222] | PubMed: 28580515 |
A novel, rapid method to compare the therapeutic windows of oral anticoagulants using the Hill coefficient [Chang JB Sci Rep, 2016, 6:29387] | PubMed: 27439480 |
A mouse bleeding model to study oral anticoagulants. [Monroe DM, et al. Thromb Res, 2014, 133 Suppl 1:S6-8] | PubMed: 24759147 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。