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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In DMSO USD 420 In stock
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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 slightly soluble or insoluble
Ethanol slightly soluble or insoluble
In vivo 30% PEG 400+0.5% Tween 80+5% Propylene glycol 30mg/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
NCT03045406 Not yet recruiting Venous Thromboembolism Fadoi Foundation, Italy|University of Perugia, Italy March 2017 Phase 3
NCT02666742 Not yet recruiting Ventricular Tachycardia Dhanunjaya Lakkireddy, MD, FACC|Bristol-Myers Squibb|University of Kansas Medical Center February 2017 Phase 4
NCT02933697 Not yet recruiting Atrial Fibrillation|End-stage Kidney Disease German Atrial Fibrillation Network|Bristol-Myers Squibb|Pfizer January 2017 Phase 3
NCT02958969 Not yet recruiting Venous Thromboembolism|Multiple Myeloma Brigham and Womens Hospital|Bristol-Myers Squibb January 2017 Phase 4
NCT02981472 Recruiting Thrombosis Bristol-Myers Squibb|Pediatric Heart Network|Pfizer January 2017 Phase 2
NCT02406885 Not yet recruiting Bariatric Surgery|Obesity Johns Hopkins University December 2016 Phase 4

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Factor Xa Signaling Pathway Map

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