For research use only.
Catalog No.S1593 Synonyms: BMS 562247-01
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.
Selleck's Apixaban has been cited by 18 publications
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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
|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.|
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.  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. 
|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%).  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.  Apixaban significantly inhibits factor Xa activity with IC50 of 0.22 μM in rabbit ex vivo.  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%). |
|In vitro||DMSO||18 mg/mL (39.17 mM)|
|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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
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Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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||--|
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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