Home Metabolism Factor Xa inhibitor Apixaban For research use only.

Apixaban

Synonyms: BMS 562247-01

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.

Apixaban Chemical Structure

Apixaban Chemical Structure

CAS No. 503612-47-3

Purity & Quality Control

Apixaban Related Products

Signaling Pathway

Factor Xa Signaling Pathways

Factor Xa Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
Caco-2 Function assay 48 hrs Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging, IC50=5.91μM ChEMBL
Caco-2 Toxicity assay 48 hrs Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay, CC50=18.07μM ChEMBL
Click to View More Cell Line Experimental Data

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
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]
Kinase Assay 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.
In Vivo
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]
Animal Research Animal Models Arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) and electrically mediated carotid arterial thrombosis (ECAT) rabbit models.
Dosages ≤3 mg/kg/h
Administration Administered via i.v.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06388239 Not yet recruiting
Healthy Volunteer
International Bio service
 August 26 2024 Phase 1
NCT05869591 Recruiting
Liver Cirrhosis
Centre Hospitalier Universitaire Vaudois
 January 18 2024 Phase 2
NCT05683808 Not yet recruiting
Glioblastoma|Astrocytoma|Venous Thromboembolism
University of Vermont Medical Center|Dartmouth-Hitchcock Medical Center|MaineHealth
 January 16 2023 Phase 2

Chemical Information & Solubility

Molecular Weight 459.5 Formula

C25H25N5O4
CAS No. 503612-47-3 SDF Download Apixaban SDF
Smiles COC1=CC=C(C=C1)N2C3=C(CCN(C3=O)C4=CC=C(C=C4)N5CCCCC5=O)C(=N2)C(=O)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 18 mg/mL ( (39.17 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

Handling Instructions

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