Catalog No.S1593 Synonyms: BMS 562247-01
Molecular Weight(MW): 459.5
Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.
Purity & Quality Control
Choose Selective Factor Xa Inhibitors
|Description||Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.|
|Features||A highly selective, reversible, and direct factor Xa inhibitor.|
Apixaban exhibits a high degree of potency, selectivity, and efficacy on Factor Xa with Ki of 0.08 nM and 0.17 nM for Human Factor Xa and Rabbit Factor Xa, respectively.  In vitro, Apixaban prolongs the clotting times of normal human plasma with the concentrations (EC2x) of 3.6 μM, 0.37 μM, 7.4 μM, and 0.4 μM, which are required respectively to double the prothrombin time (PT), modified prothrombin time (mPT), activated partial thromboplastin time (APTT) and HepTest. Besides, Apixaban shows the highest potency in human and rabbit plasma, but less potency in rat and dog plasma in both the PT and APTT assays. 
|In vivo||In the dog, Apixaban shows the excellent pharmacokinetics with very low clearance (Cl: 0.02 L kg-1 h-1), and low volume of distribution (Vdss: 0.2 L kg-1). Besides, Apixaban also exhibits a moderate half-life (T1/2: 5.8 hours) and good oral bioavailability (F: 58%).  In the arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) and electrically mediated carotid arterial thrombosis (ECAT) rabbit models, Apixaban produces dose-dependent antithrombotic effects with EC50 of 270 nM, 110 nM and 70 nM, respectively.  Apixaban significantly inhibits factor Xa activity with IC50 of 0.22 μM in rabbit ex vivo.  In chimpanzee, Apixaban also shows small volume of distribution (Vdss: 0.17 L kg-1), low systemic clearance (Cl: 0.018 L kg-1 h-1), and good oral bioavailability (F: 59%). |
|In vitro||DMSO||18 mg/mL (39.17 mM)|
|In vivo||Add solvents individually and in order:
30% PEG 400+0.5% Tween 80+5% Propylene glycol
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03045406||Not yet recruiting||Venous Thromboembolism||Fadoi Foundation, Italy|University of Perugia, Italy||March 2017||Phase 3|
|NCT02666742||Not yet recruiting||Ventricular Tachycardia||Dhanunjaya Lakkireddy, MD, FACC|Bristol-Myers Squibb|University of Kansas Medical Center||February 2017||Phase 4|
|NCT02933697||Not yet recruiting||Atrial Fibrillation|End-stage Kidney Disease||German Atrial Fibrillation Network|Bristol-Myers Squibb|Pfizer||January 2017||Phase 3|
|NCT02958969||Not yet recruiting||Venous Thromboembolism|Multiple Myeloma||Brigham and Womens Hospital|Bristol-Myers Squibb||January 2017||Phase 4|
|NCT02981472||Recruiting||Thrombosis||Bristol-Myers Squibb|Pediatric Heart Network|Pfizer||January 2017||Phase 2|
|NCT02406885||Not yet recruiting||Bariatric Surgery|Obesity||Johns Hopkins University||December 2016||Phase 4|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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