Apixaban

Catalog No.S1593 Synonyms: BMS 562247-01

Apixaban Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 420 In stock
USD 320 In stock
USD 970 In stock

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

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.
Targets
Factor Xa (human) [1]
(Cell-free assay)
Factor Xa (rabbit) [1]
(Cell-free assay)
0.08 nM(Ki) 0.17 nM(Ki)
In vitro

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. [1] 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. [2]

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%). [1] 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. [2] Apixaban significantly inhibits factor Xa activity with IC50 of 0.22 μM in rabbit ex vivo. [3] 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%). [4]

Protocol

Animal Research
+ Expand
  • Animal Models: Arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) and electrically mediated carotid arterial thrombosis (ECAT) rabbit models.
  • Formulation: Apixaban is dissolved in 10% N,N-dimethylacetamide; 30% 1,2-propanediol; 60% water.
  • Dosages: ≤3 mg/kg/h
  • Administration: Administered via i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 18 mg/mL (39.17 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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.

Chemical Information

Molecular Weight 459.5
Formula

C25H25N5O4

CAS No. 503612-47-3
Storage powder
in solvent
Synonyms BMS 562247-01

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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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Factor Xa Signaling Pathway Map

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