1. Materials information
Names
| Name | dabigatran |
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| Synonym | More Synonyms |
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Dabigatran (BIBR 953) Biological Activity
| Description | Dabigatran(BIB-953; BIBR 953ZW) is a reversible and selective, direct thrombin inhibitor (DTI) with Ki value of 4.5 nM.IC50 Value: 4.5 nM (Ki); 10 nM(Thrombin-induced platelet aggregation) [1]Target: thrombinin vitro: Dabigatran selectively and reversibly inhibited human thrombin(Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC(50): 10 nM), while showing no inhibitory effect on other platelet-stimulating agents.Thrombin generation in platelet-poor plasma (PPP), measured as the endogenous thrombin potential (ETP) was inhibited concentration-dependently (IC(50): 0.56 microM). Dabigatran demonstrated 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 PPP at concentrations of 0.23, 0.83 and 0.18 microM, respectively [1]. in vivo: Dabigatran prolonged 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). Dose- and time-dependent anticoagulant effects were observed with dabigatran etexilate administered orally to conscious rats (10, 20 and 50 mg/kg) or rhesus monkeys (1, 2.5 or 5 mg/kg), with maximum effects observed between 30 and 120 min after administration, respectively [1]. Patients treated with dabigatran etexilate experienced fewer ischaemic strokes (3.74 dabigatran etexilate vs 3.97 warfarin) and fewer combined intracranial haemorrhages and haemorrhagic strokes (0.43 dabigatran etexilate vs 0.99 warfarin) per 100 patient-years [2].Clinical trial: An Evaluation of the Pharmacokinetics and Pharmacodynamics of Oral Dabigatran Etexilate in Hemodialysis Patients . Phase1 |
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| Related Catalog | Signaling Pathways >> Metabolic Enzyme/Protease >> Thrombin Research Areas >> Cardiovascular Disease |
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| References | [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. [2]. Kansal AR, Sorensen SV, Gani R, Cost-effectiveness of dabigatran etexilate for the prevention of stroke and systemic embolism in UK patients withatrial fibrillation. Heart. 2012 Apr;98(7):573-8. |
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Chemical & Physical Properties
| Density | 1.4±0.1 g/cm3 |
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| Boiling Point | 797.1±70.0 °C at 760 mmHg |
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| Melting Point | 268-272ºC |
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| Molecular Formula | C25H25N7O3 |
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| Molecular Weight | 471.511 |
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| Flash Point | 435.9±35.7 °C |
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| Exact Mass | 471.201874 |
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| PSA | 150.22000 |
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| LogP | 0.79 |
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| Vapour Pressure | 0.0±2.9 mmHg at 25°C |
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| Index of Refraction | 1.694 |
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| Storage condition | Refrigerator, Under Inert Atmosphere |
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Synonyms
| Dabigatran |
| UNII-I0VM4M70GC |
| BIBR-953 |
| BIBR 953ZW |
| 3-[[2-[(4-carbamimidoylanilino)methyl]-1-methylbenzimidazole-5-carbonyl]-pyridin-2-ylamino]propanoic acid |
2. Packaging of materials
For powders: normal is 25kgs/Drum or bag, or larger/smaller package as request.
For liquids: normal 25kgs/drum, 180-300kgs/bucket, or IBC, determined by the nature of the product.
Or smaller package 1kg/bottle, 10kgs/bottle as request.
3. Shipping & Delivery
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Suitable for goods under 50kg
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Provide airport to airport service
Suitable for goods over 50kg
Delivery: 3-14 days
Cost: high cost
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Suitable for goods over 100kg
Delivery: 2-45 days
Cost: low cost
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