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Betrixaban

Cat. No. M2597
Betrixaban Structure
Synonym:

PRT-054021

Size Price Availability Quantity
5mg USD 120 In stock
10mg USD 190 In stock
50mg USD 670 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Betrixaban is a highly potent, selective, and orally efficacious factor Xa inhibitor with IC50 of 1.2 nM(inhibition of Factor 10a).Betrixaban is an oral direct inhibitor being developed for the prevention of venous thromboembolism (VTE).Betrixaban demonstrates antithrombotic activity and appeared well tolerated in knee replacement patients at the doses studied.

Protocol
Cell Experiment
Cell lines whole blood
Preparation method In a tissue factor-induced thrombin generation assay, betrixaban in concentrations ranging from 5 ng/mL to 25 ng/mL inhibited thrombin generation to a comparable degree as trough, and the peak levels were achieved by 2.5 mg fondaparinux.
Concentrations 5 ng/mL to 25 ng/mL
Incubation time 3–4 h
Animal Experiment
Animal models rabbit vena cava
Formulation 0.5% methylcellulose
Dosages 3 mg/kg
Administration i.v.
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 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.

Chemical Information
Molecular Weight 451.91
Formula C23H22ClN5O3
CAS Number 330942-05-7
Purity >99%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source Expert Opin Pharmacother (2013). Figure 2. Betrixaban
Method PK--PD analysis
Cell Lines
Concentrations 27.7 ng/mL and 58.6 ng/mL
Incubation Time 3.17 h
Results The median time of maximum plasma concentration (Tmax) for betrixaban occurred at 3.17 h after dosing for both dose groups
Rating
Source Expert Opin Pharmacother (2013). Figure 1. Betrixaban
Method PK--PD analysis
Cell Lines
Concentrations 27.7 ng/mL and 58.6 ng/mL
Incubation Time 3.17 h
Results The PK--PD modeling results demonstrated that betrixaban had no effect on cardiac repolarization
Rating
References

Profile of betrixaban and its potential in the prevention and treatment of venous thromboembolism
Chan NC, et al. Vasc Health Risk Manag. 2015 Jun 26;11:343-51. PMID: 26170684.

A randomized evaluation of betrixaban, an oral factor Xa inhibitor, for prevention of thromboembolic events after total knee replacement (EXPERT).
Turpie AG,et al. Thromb Haemost. 2009 Jan;101(1):68-76. PMID: 19132191.

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Rivaroxaban

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Betrixaban, PRT-054021 supplier, Factor Xa, inhibitors

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