Dabigatran Etexilate
Product Description
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Molecular Weight:
627.73 Dabigatran Etexilate 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.
Biological Activity
Protocol(Only for Reference)
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
1
References
[1] Wienen W, et al. Thromb Haemost, 2007, 98(1), 155-162.
[2] McKellar SH, et al. J Thorac Cardiovasc Surg, 2011, 141(6), 1410-1416.
[3] Wienen W, et al. Thromb Haemost, 2007, 98(2), 333-338.
Chemical Information
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Molecular Weight:
627.73 Dabigatran Etexilate 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.
Biological Activity
Description | Dabigatran Etexilate 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] | |||||
Features | |
Protocol(Only for Reference)
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species | Baboon | Dog | Monkey | Rabbit | Guinea pig | Rat | Hamster | Mouse |
Weight (kg) | 12 | 10 | 3 | 1.8 | 0.4 | 0.15 | 0.08 | 0.02 |
Body Surface Area (m2) | 0.6 | 0.5 | 0.24 | 0.15 | 0.05 | 0.025 | 0.02 | 0.007 |
Km factor | 20 | 20 | 12 | 12 | 8 | 6 | 5 | 3 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Rat dose (mg/kg) = mouse dose (22.4 mg/kg) × | mouse Km(3) | = 11.2 mg/kg |
rat Km(6) |
1
References
[1] Wienen W, et al. Thromb Haemost, 2007, 98(1), 155-162.
[2] McKellar SH, et al. J Thorac Cardiovasc Surg, 2011, 141(6), 1410-1416.
[3] Wienen W, et al. Thromb Haemost, 2007, 98(2), 333-338.
Chemical Information
Molecular Weight (MW) | 627.73 |
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Formula | C34H41N7O5 |
CAS No. | 211915-06-9 |
Storage | 3 years -20℃Powder |
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6 months-80℃in solvent (DMSO, water, etc.) | |
Synonyms | BIBR-1048 |
Solubility (25°C) * | In vitro | DMSO | 126 mg/mL (200.72 mM) |
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Water | <1 mg/mL ( | ||
Ethanol | 12 mg/mL (19.11 mM) | ||
|
Chemical Name | (E)-ethyl 3-(2-((4-(N'-(hexyloxycarbonyl)carbamimidoyl)phenylamino)methyl)-1-methyl-N-(pyridin-2-yl)-1H-benzo[d]imidazole-5-carboxamido)propanoate |
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Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
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Mass(mg) | 0.62773 | 6.2773 | 12.5546 | 18.8319 |
Contact us if you need more details on 211915-06-9. We are ready to answer your questions on packaging, logistics, certification or any other aspects about Dabigatran Etexilate 211915-06-9、211915-06-9 Dabigatran Etexilate. If these products fail to match your need, please contact us and we would like to provide relevant information.
Product Categories : Others > Thrombin Inhibitor
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