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.

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Cited by 11 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.

Purity & Quality Control

Choose Selective Factor Xa Inhibitors

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:[2]
+ 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 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.
30mg/mL

* 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
NCT03854149 Not yet recruiting Congenital Heart Disease|Atrial Fibrillation|Thromboembolism|Anticoagulants Causing Adverse Effects in Therapeutic Use AHEPA University Hospital|Onassis Cardiac Surgery Centre|Attikon Hospital|MITERA Children''s Hospital June 2019 --
NCT03854149 Not yet recruiting Congenital Heart Disease|Atrial Fibrillation|Thromboembolism|Anticoagulants Causing Adverse Effects in Therapeutic Use AHEPA University Hospital|Onassis Cardiac Surgery Centre|Attikon Hospital|MITERA Children''s Hospital June 2019 --
NCT03864406 Recruiting Healthy Volunteers National Institutes of Health Clinical Center (CC) March 28 2019 Phase 1
NCT03864406 Recruiting Healthy Volunteers National Institutes of Health Clinical Center (CC) March 28 2019 Phase 1
NCT03590743 Recruiting Deep Vein Thrombosis Mayo Clinic|Bristol-Myers Squibb|Pfizer February 19 2019 Phase 4
NCT03590743 Recruiting Deep Vein Thrombosis Mayo Clinic|Bristol-Myers Squibb|Pfizer February 19 2019 Phase 4

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Factor Xa Signaling Pathway Map

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