Catalog No.S1593

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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Apixaban Chemical Structure

Apixaban Chemical Structure
Molecular Weight: 459.5

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Apixaban is available in the following compound libraries:

Product Information

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  • Research Area
  • Apixaban Mechanism

Product Description

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.
Targets Factor Xa (human) [1]
(Cell-free assay)
Factor Xa (rabbit) [1]
(Cell-free assay)
IC50 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]
Features A highly selective, reversible, and direct factor Xa inhibitor.

Protocol(Only for Reference)

Kinase Assay: [1]

Enzyme Affinity Assays. All enzyme Ki values are obtained from purified human enzymes. All fXa assays are run in microtiter plates using a total volume of 250 μL in 0.1 M sodium phosphate buffer containing 0.2 M NaCl and 0.5% polyethylene glycol 6000 at pH 7.0. Apixaban are run at 10 μM, 3.16 μM, 1.0 μM, 0.316 μM, 0.1 μM, 0.0316 μM, 0.01 μM, and 0.00316 μM. Plates are read for 30 minutes at 405 nm. Rates are determined in the presence of the controls (no inhibitor) and for the inhibitors. Apixaban are tested in duplicate studies and are compared with the same internal standards. The intraassay and interassay variabilities are 5% and 20%, respectively. All of the enzyme assays are conducted in pH 7.4 buffer at room temperature. All enzymes are purified from human tissues and are obtained from commercially available sources. Individual enzyme and substrate Km are determined in separate experiments and are close to values established in the literature. Steady-state inhibition of enzyme activity is determined by incubating a range of inhibitor concentrations (1 nM to 50 μM, in duplicate) with fixed enzyme (0.1 nM−100 nM) and peptide substrate (200 μM−1000 μM) concentration for up to 30 minutes. The Ki is calculated, assuming competitive inhibition and one-site binding, either from the IC50 or from the extent of inhibition at each inhibitor concentration.

Animal Study: [2]

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Pinto DJ, et al. J Med Chem. 2007, 50(22), 5339-5356.

[2] Wong PC, et al. J Thromb Haemost. 2008, 6(5), 820-829.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02809469 Not yet recruiting Atrial Fibrillation Hamilton Health Sciences Corporation|Population Health Re  ...more 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|Univ  ...more 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 Outcome  ...more Alliance Foundation Trials, LLC.|Patient-Centered Outcomes Research Institute June 2016 --

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Chemical Information

Download Apixaban SDF
Molecular Weight (MW) 459.5


CAS No. 503612-47-3
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms BMS 562247-01
Solubility (25°C) * In vitro DMSO 18 mg/mL (39.17 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 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.
Chemical Name 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

Tech Support

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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