Size | Price | Stock | Qty |
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100mg |
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250mg |
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500mg |
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1g |
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2g |
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5g |
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Other Sizes |
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Purity: ≥98%
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.
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].
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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].
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Animal Protocol |
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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 |
Molecular Formula |
C25H25N5O4
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Molecular Weight |
459.5
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CAS # |
503612-47-3
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SMILES |
O=C(C1=NN(C2=CC=C(OC)C=C2)C3=C1CCN(C4=CC=C(N5C(CCCC5)=O)C=C4)C3=O)N
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Chemical Name |
1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5-dihydropyrazolo[5,4-c]pyridine-3-carboxamide
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Synonyms |
BMS56224701; BMS 56224701; BMS 562247-01; Apixaban, BMS-56224701; brand name: Eliquis
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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)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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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.
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.
Plot of apixaban inhibition of human FXa activity at different concentrations of the chromogenic peptide substrate S‐2765.J Thromb Haemost.2008 May;6(5):820-9. th> |
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Antithrombotic effects in the arteriovenous‐shunt thrombosis (AVST) and venous thrombosis (VT) rabbit models.J Thromb Haemost.2008 May;6(5):820-9. td> |
Antithrombotic effects in the rabbit model of electrically mediated carotid arterial thrombosis.J Thromb Haemost.2008 May;6(5):820-9. td> |