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.
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3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
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|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||30% PEG400+0.5% Tween80+5% propylene glycol||30 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02809469||Not yet recruiting||Atrial Fibrillation||Hamilton Health Sciences Corporation|Population Health Research Institute||August 2016||Phase 2|
|NCT02829957||Not yet recruiting||Venous Thromboembolism|Menstruation||Indiana University||August 2016||Phase 2|
|NCT02666742||Not yet recruiting||Ventricular Tachycardia||Dhanunjaya Lakkireddy, MD, FACC|Bristol-Myers Squibb|University of Kansas Medical Center||July 2016||Phase 4|
|NCT02836457||Not yet recruiting||Venous Thromboembolism||Bristol-Myers Squibb||July 2016||--|
|NCT02744092||Not yet recruiting||Cancer|Venous Thromboembolism|Deep Vein Thrombosis (DVT)|Pulmonary Embolism (PE)|Blood Clot|VTE||Alliance Foundation Trials, LLC.|Patient-Centered Outcomes Research Institute||June 2016||--|
|NCT02664155||Not yet recruiting||Renal Insufficiency||Centre Hospitalier Universitaire de Saint Etienne||June 2016||Phase 3|
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