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Apixaban

Catalog No.S1593
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Apixaban Chemical Structure

  • BMS-740808

    BMS-740808 is a highly potent, selective, efficacious, and orally bioavailable blood coagulation factor Xa inhibitor with a Ki of 30 pM.

  • Rivaroxaban (Xarelto)

    Rivaroxaban (Xarelto, BAY 59-7939) is an oral, direct inhibitor of Factor Xa with a Ki of 0.4 nM and an IC50 of 0.7 nM for purified human FXa.

  • LY315920(Varespladib)

    LY315920(Varespladib) is a sPLA2 inhibitor (IC50 of 9.6 ±1 nM)

  • Abiraterone (CB-7598)

    Abiraterone (CB-7598) is a potent steroidal cytochrome P450 17alpha-hydroxylase-17,20-lyase (CYP17) inhibitor with an IC50 at 4 nM.

  • TAK-700 (Orteronel)

    Inhibitor of the 17,20 lyase.

  • Cilostazol

    Cilostazol is a medication used in the alleviation of the symptom of intermittent claudication in individuals with peripheral vascular disease.

  • Isotretinoin

    It was developed to be used as a chemotherapy medication for the treatment of brain cancer, pancreatic cancer and more.

  • Trilostane

    Trilostane is an inhibitor of 3 β-hydroxysteroid dehydrogenase used in the treatment of Cushing’s syndrome.

  • Sildenafil citrate

    Sildenafil citrate is an agent used to treat erectile dysfunction and pulmonary arterial hypertension (PAH).

  • Voriconazole

    Voriconazole (VFEND) is a triazole antifungal medication that is generally used to treat serious, invasive fungal infections.

Biological Activity

Apixaban is a direct factor Xa inhibitor with an IC50 of 0.22±0.02 µM. It is a compound being investigated as an anticoagulant. Apixaban has similar affinity for human and rabbit factor Xa (FXa). Rabbits are commonly used in development of thrombosis disease models; however, unlike in other species, apixaban demonstrated poor oral bioavailability (F = 3%) and a high clearance rate in rabbits. Oxidative metabolism of [14C] apixaban by liver microsomes was approximately 20 times faster in rabbits than in rats or humans. [1][2]

References on Apixaban
  • [1] http://en.wikipedia.org/wiki/Apixaban ;
  • [2] J Thromb Thrombolysis. 2010 Jan;29(1):70-80.
Molecular Weight (WM): 459.5
Formula:

C25H25N5O4

CAS No.: 503612-47-3
Synonyms:
N/A
Dissolve in (25°C): DMSO ≥18mg/mL 
Water <1mg/mL 
Ethanol <1mg/mL 
Storage: 2 years-20°CPowder
1 week-4°Cin DMSO
1 month-80°in DMSO

Quality Control & MSDS

View current batch:
COA H-NMR

Research Area

Related Inhibitors

Recommended Screening Libraries

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