Name: Betrixaban
Price: 286.00 USD

- Overview
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    Background
    
    Betrixaban is a highly potent, selective, and orally efficacious inhibitor of factor Xa with IC50 value of 1.5nM [1].Betrixaban shows excellent anticoagulant potency in vitro. In the rabbit deep vein thrombosis model, the concentration of betrixaban required to double the rabbit prothrombin time is below 2μM. Betrixaban is selective for fXa and has poor activity for thrombin, trypsin, t-PA and aPC. The patch clamp hERG assay shows that betrixaban has low affinity with hERG suggesting it is safer than other candidate compounds. In addition, betrixaban displays a profile of good oral bioavailability and oral exposure, long half-life in animal models. It has bioavailability of 51.6% at dose of 0.5 mg/kg IV and 2.5 mg/kg PO. Furthermore, the Phase II study has proved betrixaban as an oral fXa inhibitor for prevention of venous thromboembolic events [1].
    
    [1] Zhang P, Huang W, Wang L, Bao L, Jia ZJ, Bauer SM, Goldman EA, Probst GD, Song Y, Su T, Fan J, Wu Y, Li W, Woolfrey J, Sinha U, Wong PW, Edwards ST, Arfsten AE, Clizbe LA, Kanter J, Pandey A, Park G, Hutchaleelaha A, Lambing JL, Hollenbach SJ, Scarborough RM, Zhu BY. Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2179-85.
- Properties
  - Alternative Name
    
    N-(5-chloropyridin-2-yl)-2-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]-5-methoxybenzamide
    
    CAS Number
    
    330942-05-7
    
    Molecular Formula
    
    C23H22ClN5O3
    
    Molecular Weight
    
    451.91
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥45.2 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

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Betrixaban

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