Apixaban

• Description :

  Apixaban (BMS-562247-01) is a highly selective, reversible and orally active inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively[1]. Apixaban is in development for the prevention and treatment of various thromboembolic diseases[2].

• CAS Number :

  [503612-47-3]

• Product Name Alternative :

  BMS-562247-01

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H315, H320, H335

• Target :

  Factor Xa

• Type :

  Reference compound

• Related Pathways :

  Metabolic Enzyme/Protease

• Applications :

  COVID-19-immunoregulation

• Field of Research :

  Cardiovascular Disease; Cancer

• Assay Protocol :

  https://www.medchemexpress.com/Apixaban.html

• Purity :

  99.99

• Solubility :

  DMSO : 50 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL

• Smiles :

  NC(C1=NN(C2=C1CCN(C2=O)C3=CC=C(C=C3)N4CCCCC4=O)C5=CC=C(C=C5)OC)=O

• Molecular Formula :

  C25H25N5O4

• Molecular Weight :

  459.50

• Precautions :

  H302, H315, H320, H335

• References & Citations :

  [1]Pinto DJ, et al. Discovery of 1- (4-methoxyphenyl) -7-oxo-6- (4- (2-oxopiperidin-1-yl) phenyl) -4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa. J Med Chem. 2007 Nov 1;50 (22) :5339-56.|[2]Wong PC, et al. Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studies. J Thromb Haemost. 2008 May;6 (5) :820-9|[3]Zhang D, et al. Metabolism, pharmacokinetics and pharmacodynamics of the factor Xa inhibitor apixaban in rabbits. J Thromb Thrombolysis. 2010 Jan;29 (1) :70-80|[4]He K, et al. Preclinical pharmacokinetics and pharmacodynamics of apixaban, a potent and selective factor Xa inhibitor. Eur J Drug Metab Pharmacokinet. 2011 Sep;36 (3) :129-39

• Shipping Conditions :

  Blue Ice

• Storage Conditions :

  -20°C (Powder, protect from light)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Launched