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BIBR 953

Cat. No. M1674
BIBR 953 Structure
Synonym:

Dabigatran, Pradaxa

Size Price Availability Quantity
Free Sample 0.5 mg  USD 0 In stock
5mg USD 80  USD80 In stock
10mg USD 140  USD140 In stock
50mg USD 460  USD460 In stock
100mg USD 720  USD720 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

BIBR 953 (Dabigatran, Pradaxa) is a highly selective, reversible, and potent thrombin inhibitor and is orally available as the prodrug, dabigatran etexilate. It has shown antithrombotic efficacy in animal models of thrombosis, with a rapid onset of action and predictable pharmacodynamic response.

Protocol
Cell Experiment
Cell lines
Preparation method Human thrombin is dose-dependently and competitively inhibited by dabigatran (Table 2). This inhibition with a Ki of 4.5 nmol/L compares well to the Ki of melagatran (11.2 nmol/L). Real-time binding kinetics using surface plasmon resonance showed a rapid and reversible binding of dabigatran to thrombin.7 The concentration of dabigatran required tom double the in vitro coagulation time (EC2) in platelet poor plasma is species dependent and varies with the type of test (Table 3).
Concentrations
Incubation time
Animal Experiment
Animal models rabbit model of venous thrombosis
Formulation saline
Dosages a single IV administration of 5, 10, 20, and 30 mg/kg
Administration i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 471.51
Formula C25H25N7O3
CAS Number 211914-51-1
Purity >99%
Solubility DMSO
Storage at -20°C
References

[1] Blech et al. Drug Metab Dispos. The metabolism and disposition of the oral direct thrombin inhibitor, dabigatran, in humans.

[2] Trocóniz et al. J Clin Pharmacol. Population pharmacokinetic analysis of the new oral thrombin inhibitor dabigatran etexilate (BIBR 1048) in patients undergoing primary elective total hip replacement surgery.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BIBR 953, Dabigatran, Pradaxa supplier, Thrombopoietin/Thrombin, inhibitors

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