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Synonyms: BIBR 953ZW, BIBR 953
| Description | Dabigatran (BIBR 953ZW) is a THROMBIN inhibitor which acts by binding and blocking thrombogenic activity and the prevention of thrombus formation. It is used to reduce the risk of stroke and systemic EMBOLISM in patients with nonvalvular atrial fibrillation. |
| Targets & IC50 | Thrombin:9.3 nM |
| In vitro | Dabigatran is a very potent anticoagulant. Dabigatran shows that the terminal phenyl can be substituted by the more hydrophilic 2-pyridyl group without substantial loss of activity. Dabigatran inhibits thrombin, plasmin, factor Xa, trypsin, tPA and activated protein C with Ki of 4.5 nM, 1.7 μM, 3.8 μM, 50 nM, 45 μM and 20 μM, respectively. [1] Dabigatran specifically and reversibly inhibits thrombin. [2] |
| In vivo | Dabigatran exhibits the most favorable activity profile following i.v. administration to rats. [1] The bioavailability of dabigatran after p.o. administration of dabigatran etexilate is 7.2%. Dabigatran is predominantly excreted in the feces after p.o. treatment and in the urine after i.v. treatment. The mean terminal half-life of dabigatran is approximately 8 hours. Dabigatran acylglucuronides accounts for 0.4% and 4% of the dose in urine after p.o. and i.v. dosing, respectively. [3] |
| Synonyms | BIBR 953ZW, BIBR 953 |
| Molecular Weight | 471.51 |
| Formula | C25H25N7O3 |
| Cas No. | 211914-51-1 |
| Smiles | Cn1c(CNc2ccc(cc2)C(N)=N)nc2cc(ccc12)C(=O)N(CCC(O)=O)c1ccccn1 |
| Relative Density. | 1.38 g/cm3 (Predicted) |
| Storage | Store at low temperature,Keep away from direct sunlight Pure form: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: < 1 mg/mL (insoluble or slightly soluble) H2O: < 0.1 mg/mL (insoluble) 0.1M HCL: 20.6 mg/mL (43.69 mM)  | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
0.1M HCL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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