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Formula | C25H25N5O4 |
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Molecular Weight | 459.5 | CAS No. | 503612-47-3 | |
Solubility (25°C)* | In vitro | DMSO | 47 mg/mL (102.28 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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. | ||||
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Targets |
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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] |
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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] |
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Features | A highly selective, reversible, and direct factor Xa inhibitor. |
Kinase Assay: |
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Animal Study: |
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Data from [Data independently produced by , , Sci Rep, 2016, 6:29387]
Data from [Data independently produced by , , Neuroscience, 2018, 371:445-454]
Engineering and evaluation of FXa bypassing agents that restore hemostasis following Apixaban associated bleeding [ Nat Commun, 2024, 15(1):3912] | PubMed: 38724509 |
Detection of direct oral anticoagulants with the diluted Russel's viper venom time [ Int J Lab Hematol, 2024, 10.1111/ijlh.14300] | PubMed: 38721750 |
Rivaroxaban attenuates neutrophil maturation in the bone marrow niche [ Basic Res Cardiol, 2023, 118(1):31] | PubMed: 37580509 |
OKL-1111, A modified cyclodextrin as a potential universal reversal agent for anticoagulants [ Thromb Res, 2023, 227:17-24] | PubMed: 37207560 |
Factor VII, EPCR, aPC Modulators: novel treatment for neuroinflammation [ J Neuroinflammation, 2022, 19(1):138] | PubMed: 35690769 |
Evaluation of Xa inhibitors as potential inhibitors of the SARS-CoV-2 Mpro protease [ PLoS One, 2022, 17(1):e0262482] | PubMed: 35015795 |
In vitro reversal of direct factor Xa inhibitors: Direct comparison of andexanet alfa and prothrombin complex concentrates Cofact and Beriplex/Kcentra [ Res Pract Thromb Haemost, 2022, 6(5):e12775] | PubMed: 35928523 |
Markers for neural degeneration and regeneration: novel highly sensitive methods for the measurement of thrombin and activated protein C in human cerebrospinal fluid [ Neural Regen Res, 2021, 16(10):2086-2092] | PubMed: 33642398 |
An engineered factor Va prevents bleeding induced by direct-acting oral anticoagulants by different mechanisms [ Blood Adv, 2020, 4(15):3716-3727] | PubMed: 32777068 |
A Novel Highly Sensitive Method for Measuring Inflammatory Neural-Derived APC Activity in Glial Cell Lines, Mouse Brain and Human CSF [ Int J Mol Sci, 2020, 31;21(7):2422] | PubMed: 32244492 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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