Apixaban (BMS-56224701)

Alias: BMS56224701; BMS 56224701; BMS 562247-01; Apixaban, BMS-56224701; brand name: Eliquis
Cat No.:V0949 Purity: ≥98%
Apixaban (formerlyBMS56224701; BMS 56224701;BMS-56224701; trade name: Eliquis),an approved drug used to treat and prevent the formation of blood clots, is a highly selective, reversible, direct inhibitor of Factor Xa with potential anti-coagulant activity.
Apixaban (BMS-56224701) Chemical Structure CAS No.: 503612-47-3
Product category: Factor Xa
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
100mg
250mg
500mg
1g
2g
5g
Other Sizes

Other Forms of Apixaban (BMS-56224701):

  • Apixaban 13CD3
  • Apixaban-d3 (Apixaban-d3; BMS-562247-01-d3)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Apixaban (formerly BMS56224701; BMS 56224701; BMS-56224701; trade name: Eliquis), an approved drug used to treat and prevent the formation of blood clots, is a highly selective, reversible, direct inhibitor of Factor Xa with potential anti-coagulant activity. It inhibits Factor Xa with a Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively. Apixaban is used as an anticoagulant for the treatment of venous thromboembolic events. Factor Xa is the activated form of the coagulation factorthrombokinase. Inhibiting Factor Xa could offer an alternate method for anticoagulation. Direct Xa inhibitors are popular anticoagulants. Apixaban was approved in Europe in 2012 and in the U.S. in 2014 for treatment and secondary prophylaxis of deep vein thrombosis (DVT) and pulmonary embolism (PE). It was developed in a joint venture by Pfizer and Bristol-Myers Squibb.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
At concentrations (EC2x) of 3.6 μM, 0.37 μM, 7.4 μM, and 0.4 μM, respectively, apixaban (BMS-562247-01) prolongs the clotting times of normal human plasma, which is needed to double the prothrombin time (PT), modified prothrombin time (mPT), activated partial thromboplastin time (APTT), and HepTest. Furthermore, in both the PT and APTT tests, Apixaban exhibits the highest potency in human and rabbit plasma but less potency in rat and dog plasma[2].
ln Vivo
In dogs, Apixaban (BMS-562247-01) has good pharmacokinetics with a very low volume of distribution (Vdss: 0.2 L/kg) and a very low clearance (Cl: 0.02 L/kg/h). Additionally, Apixaban has a decent oral bioavailability (F: 58%) and a reasonable half-life (T1/2: 5.8 hours)[1]. Apixaban exhibits dose-dependent antithrombotic effects in rabbit models of arteriovenous shunt thrombosis (AVST), venous thrombosis (VT), and electronically mediated carotid arterial thrombosis (ECAT) with EC50 values of 270 nM, 110 nM, and 70 nM, respectively[2]. In rabbits ex vivo, apixaban dramatically reduces factor Xa activity with an IC50 of 0.22 μM[3]. Apixaban also exhibits low systemic clearance (Cl: 0.018 L/kg/h), a modest volume of distribution (Vdss: 0.17 L/kg), and good oral bioavailability (F: 59%) in chimpanzees[4].
Animal Protocol
Dssolved in 10% N,N-dimethylacetamide; 30% 1,2-propanediol; 60% water; ≤3 mg/kg/h; i.v. injection
Arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) and electrically mediated carotid arterial thrombosis (ECAT) rabbit models
References
[1]. Pinto DJ, et al. Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blo
[2]. Wong PC, et al. Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studies. J Thromb Haemost. 2008 May;6(5):820-9
[3]. Zhang D, et al. Metabolism, pharmacokinetics and pharmacodynamics of the factor Xa inhibitor apixaban in rabbits. J Thromb Thrombolysis. 2010 Jan;29(1):70-80
[4]. He K, et al. Preclinical pharmacokinetics and pharmacodynamics of apixaban, a potent and selective factor Xa inhibitor. Eur J Drug Metab Pharmacokinet. 2011 Sep;36(3):129-39
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C25H25N5O4
Molecular Weight
459.5
CAS #
503612-47-3
SMILES
O=C(C1=NN(C2=CC=C(OC)C=C2)C3=C1CCN(C4=CC=C(N5C(CCCC5)=O)C=C4)C3=O)N
Chemical Name
1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5-dihydropyrazolo[5,4-c]pyridine-3-carboxamide
Synonyms
BMS56224701; BMS 56224701; BMS 562247-01; Apixaban, BMS-56224701; brand name: Eliquis
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 18 mg/mL (39.2 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Solubility (In Vivo)
30% PEG400+0.5% Tween80+5% propylene glycol:30 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.1763 mL 10.8814 mL 21.7628 mL
5 mM 0.4353 mL 2.1763 mL 4.3526 mL
10 mM 0.2176 mL 1.0881 mL 2.1763 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • Apixaban

    Plot of apixaban inhibition of human FXa activity at different concentrations of the chromogenic peptide substrate S‐2765.2008 May;6(5):820-9.

  • Apixaban

    Antithrombotic effects in the arteriovenous‐shunt thrombosis (AVST) and venous thrombosis (VT) rabbit models.2008 May;6(5):820-9.

  • Apixaban

    Antithrombotic effects in the rabbit model of electrically mediated carotid arterial thrombosis.2008 May;6(5):820-9.

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