For research use only.

Catalog No.S1593 Synonyms: BMS 562247-01

18 publications

Apixaban Chemical Structure

CAS No. 503612-47-3

Apixaban (BMS 562247-01) 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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Selleck's Apixaban has been cited by 18 publications

2 Customer Reviews

  • The peak fluorescence of each time course at the specified drug concentration are plotted as a function of concentration of apixaban. Dose-response curve was fitted to the Hill equation.

    Sci Rep, 2016, 6:29387. Apixaban purchased from Selleck.

  • FXa inhibitor, apixaban, decreased thrombin levels after sciatic injury. Thrombin activity in mice sciatic nerve (A) Nerves were subjected to crush injury, 1 h after injury sciatic nerves were excised from the injured (black) and contralateral uninjured nerve (white). Nerves were placed in 96-well black microplate in buffer, with or without apixaban (10 µM). Thrombin levels decreased significantly in the wells that contained apixaban. A two-way ANOVA indicated that apixaban significantly reduced the thrombin activity both in the uninjured and injured sides (F(1,35) = 19.276, p = 0.001 (uninjured n = 6, uninjured + apixaban n = 8, injured n = 18, injured + apixaban n = 8). (B) Thrombin activity 1 h after nerve injury in mice treated with apixaban (20 mg/kg). Thrombin levels were decreased significantly in mice that were treated with apixaban both in the uninjured (white) and injured (black) nerves (F(1,28) = 11.052, p = 0.02 by a two-way ANOVA) (uninjured n = 7, uninjured + apixaban n = 9, injured n = 7, injured + apixaban n = 9). (C) No significant effect on thrombin levels remained 1 day after a single apixaban injection (uninjured n = 18, uninjured + apixaban n = 8, injured n = 4, injured + apixaban n = 8).

    Neuroscience, 2018, 371:445-454. Apixaban purchased from Selleck.

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Choose Selective Factor Xa Inhibitors

Biological Activity

Description Apixaban (BMS 562247-01) 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.
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]


Animal Research:[2]
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  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 18 mg/mL (39.17 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG 400+0.5% Tween 80+5% Propylene glycol
For best results, use promptly after mixing.

* 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


CAS No. 503612-47-3
Storage powder
in solvent
Synonyms BMS 562247-01
Smiles COC1=CC=C(C=C1)N2C3=C(CCN(C3=O)C4=CC=C(C=C4)N5CCCCC5=O)C(=N2)C(=O)N

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04344717 Not yet recruiting Drug: Apixaban single dose Short Bowel Syndrome|Anticoagulation Universitaire Ziekenhuizen Leuven September 2020 Phase 4
NCT04278729 Not yet recruiting Drug: Apixaban 5 MG Nephrotic Syndrome|Membranous Nephropathy University of North Carolina Chapel Hill|American College of Clinical Pharmacy August 2020 Phase 1
NCT04435769 Not yet recruiting -- Atrial Fibrillation Pfizer July 1 2020 --
NCT03812835 Not yet recruiting -- Thrombosis Deep Vein|Pulmonary Embolism Pfizer July 1 2020 --

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Factor Xa Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID