Apixaban

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].

Product Specifications

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