Apixaban
Based on 13 publication(s) in Google Scholar
Apixaban (BMS-562247-01) is a highly selective, reversible and orally active inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively. Apixaban is in development for the prevention and treatment of various thromboembolic diseases.
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- Pureté: 99.99%
- CAS No.: 503612-47-3
- Formule: C25H25N5O4
- Masse moléculaire:459.50
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
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Publications Citing Use of MedChemExpress (MCE) Apixaban
More- Nature. 2026 Jun 24.
- Biomaterials. 2026 Feb:325:123600. [Abstract]
- Cell Death Dis. 2025 Feb 19;16(1):109. [Abstract]
- Molecules. 2023 Feb 28;28(5):2254. [Abstract]
- Sci Rep. 2020 Jul 6;10(1):11079. [Abstract]
- Res Pract Thromb Haemost. 2020 Oct 25;4(8):1269-1281. [Abstract]
- J Chem Thermodyn. 2020 May.
- Drug Metab Pharmacokinet. 2023 Dec:53:100498. [Abstract]
- Int J Lab Hematol. 2020 Apr;42(2):126-133. [Abstract]
- LabMed. 2024 Nov 18.
- Elife. 2022 Mar 23:11:e77444. [Abstract]
- Personalized Medicine Universe. 2019 May.
- Patent. US20170224812A1.
Customer Validation & Images
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In Vivo Imaging
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
Activité biologique
IC50: 0.08 nM (Human Factor Xa), 0.17 nM (Rabbit Factor Xa)
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Cell Line
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Type | Value | Description | References |
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| Caco-2 | CC50 |
18.07 μM
Compound: APIXABAN
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Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
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10.21203/rs.3.rs-23951/v1 |
| Caco-2 | IC50 |
5.91 μM
Compound: APIXABAN
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Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
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10.21203/rs.3.rs-23951/v1 |
| Platelet | EC50 |
0.07 μM
Compound: Apixaban
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Inhibition of tissue factor induced platelet activation in 76% human blood incubated for 15 mins by CD62 antibody based assay
Inhibition of tissue factor induced platelet activation in 76% human blood incubated for 15 mins by CD62 antibody based assay
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[PMID: 36462436] |
Apixaban (BMS-562247-01) 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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), low systemic clearance (Cl: 0.018 L/kg/h), and good oral bioavailability (F: 59%)[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 503612-47-3
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Appearance Solid
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Masse moléculaire 459.50
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Formule C25H25N5O4
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Color White to off-white
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SMILES
NC(C1=NN(C2=C1CCN(C2=O)C3=CC=C(C=C3)N4CCCCC4=O)C5=CC=C(C=C5)OC)=O
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Synonyms
BMS-562247-01
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (13)
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Journal Impact Factor
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Most Recent
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Biomaterials
Self-adaptive covalent coating for vascular stents: Coordinated coagulation-inflammation regulation to support re-endothelialization for atherosclerosis control. [Abstract]2026 Feb:325:123600. PMID: 40753783 -
Cell Death Dis
2025 Feb 19;16(1):109. PMID: 39971938
Apixaban purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Feb 19;16(1):109. [Abstract]
NET formation in the liver vasculature of wild-type mice was assessed by SD-IVM (spinning-disk intravital microscopy) 4 h after RgpA injection, following a single intraperitoneal administration of Apixaban (25 mg/kg) 30 min before RgpA. The formation of NETs was abolished in mice treated with apixaban.
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Molecules
Generic Methods for Simultaneous Analysis of Four Direct Oral Anticoagulants in Human Plasma and Urine by Ultra-High Performance Liquid Chromatography-Tandem Mass Spectrometry. [Abstract]2023 Feb 28;28(5):2254. PMID: 36903499 -
Sci Rep
2020 Jul 6;10(1):11079. PMID: 32632109 -
Res Pract Thromb Haemost
Effect of anticoagulants on fibrin clot structure: A comparison between vitamin K antagonists and factor Xa inhibitors. [Abstract]2020 Oct 25;4(8):1269-1281. PMID: 33313466
Apixaban purchased from MedChemExpress. Usage Cited in: Res Pract Thromb Haemost. 2020 Oct 25;4(8):1269-1281. [Abstract]
Fibrin clot polymerization turbidity and clotting lag time were measured in plasma (diluted 1:6 before testing) containing Apixaban (128 ng/mL). Clotting was initiated by tissue factor and continuously monitored for 1 h at 37 °C. Apixaban prolonged the clotting lag time by approximately 1.8-fold.
Apixaban purchased from MedChemExpress. Usage Cited in: Res Pract Thromb Haemost. 2020 Oct 25;4(8):1269-1281. [Abstract]
Fibrin clot networks and fiber density were assessed by laser scanning confocal microscopy after clotting of plasma (diluted 1:6 before testing) containing Apixaban (128 ng/mL) was initiated with tissue factor and clots were allowed to form for 2 h at room temperature. Apixaban reduced fibrin fiber density from 89 ± 7 to 78 ± 7 fibers/200 μm compared with the control.
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Drug Metab Pharmacokinet
Involvement of multiple cytochrome P450 isoenzymes in drug interactions between ritonavir and direct oral anticoagulants. [Abstract]2023 Dec:53:100498. PMID: 37778107
Apixaban purchased from MedChemExpress. Usage Cited in: Drug Metab Pharmacokinet. 2023 Dec:53:100498. [Abstract]
Apx (Apixaban; 8 μM; 20 min) was incubated with human liver microsomes, and the remaining hydroxylation and O-demethylation activities were assessed under different CYP isoenzyme inhibition conditions. The percentage remaining activity of Apx hydroxylation was 19.7 and 0% at 0.33 and 10 μM RTV, respectively. Conversely, the percentage remaining activities of Apx O-demethylation were 86.6 and 28.0% at 0.33 and 10 μM RTV, respectively.
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Int J Lab Hematol
Differential effects of direct factor IIa and factor Xa inhibitors in protein C-deficient plasma detected using thrombin generation and viscoelastometry assays. [Abstract]2020 Apr;42(2):126-133. PMID: 31756037
Apixaban purchased from MedChemExpress. Usage Cited in: Int J Lab Hematol. 2020 Apr;42(2):126-133. [Abstract]
Thrombin generation was stimulated with tissue factor and phospholipids and monitored for 60 min in control or protein C-deficient plasma preincubated with Apixaban (100-1000 nM; 5 min pretreatment + co-incubation with tissue factor/phospholipids for 10 min + continued incubation during 60 min thrombin-generation monitoring), with representative traces, endogenous thrombin potential, peak thrombin concentration, thrombin concentration at 60 min and lag time assessed.
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Elife
2022 Mar 23:11:e77444. PMID: 35294338 -
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Solvant et solubilité
DMSO : 50 mg/mL (108.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.44 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
Purified FXa is obtained after activation with Russell’s viper venom followed by affinity chromatography. The resulting FXa is > 95% pure as judged by sodium dodecylsulfate polyacrylamide gel electrophoresis. The substrate affinity values for FXa, expressed as the Michaelis-Menten-Henri constant (Km), for human, rabbit, rat and dog FXa are determined using the chromogenic substrate S-2765, and are 36, 60, 240 and 70 μM, respectively. The substrate hydrolysis is monitored by measuring absorbance at 405 nm at 25°C for up to 30 min using a SpectraMax 384 Plus plate reader and SoftMax. FXa activity for each substrate and inhibitor concentration pair is determined in duplicate. The Ki values are calculated by non-linear least-squares fitting of the steady-state substrate hydrolysis rates to the equation for competitive inhibition (Equation 1) using GRAFIT, where v equals reactions velocity in OD min−1, Vmax equals maxiumum reaction velocity, S equals substrate concentration, and I equals inhibitor concentration.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Briefly, male New Zealand White rabbits are anesthetized with ketamine (50 mg/kg i.m.) and xylazine (10 mg/kg i.m.), and their femoral artery, jugular vein and femoral vein are catheterized. Thrombosis is induced by an arteriovenous (AV)-shunt device containing a silk thread. Blood flowed from the femoral artery via the AV shunt into the opposite femoral vein for 40 min. The shunt is then disconnected and the silk thread covered with thrombus is weighed. As apixaban has an oral bioavailability of < 5% in rabbits (unpublished result), it is administered intravenously for in vivo studies. To achieve a stable plasma level with minimum experimental variability, apixaban, fondaparinux or vehicle is given by a continuous intravenous infusion 1 h prior to shunt placement. The infusion is continued throughout the experiment. Warfarin or vehicle is dosed orally once daily for 4 days. On the fourth day after the last oral dose of warfarin or vehicle, rabbits are anesthetized 1.5 h later, and the treatment effect is evaluated about 2 h postdose. Arterial blood samples for the determination of clotting times or plasma levels are collected 20 min after shunt placement. Plasma levels of apixaban are measured by a specific and sensitive liquid chromatographic mass spectrometry method (LC/MS/MS). In rabbits treated with apixaban, fondaparinux or warfarin, the antithrombotic effects of these agents are expressed as percentage inhibition of thrombus formation based on the treated vs. the corresponding mean vehicle. The ED50 value (dose that produced 50% inhibition of thrombus formation) is determined as described below. The apixaban group treatment consists of vehicle (10%N,N-dimethylacetamide; 30% 1,2-propanediol; 60% water) (n=4), and apixaban (mg/kg/h) at 0.03 (n=7), 0.1 (n=7), 0.3 (n=7), 1 (n=7), and 3 (n=3). The fondaparinux group treatment consists of vehicle (saline) (n=6), and fondaparinux (mg/kg/h1) at 0.01 (n=5), 0.03 (n=5), 0.1 (n=5), 0.3 (n=5), and 1 (n=5). The warfarin group treatment consists of vehicle (water) (n=6), and warfarin (mg/kg/day) at 0.1 (n=6), 0.3 (n=6), 1 (n=6), and 3 (n=6).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (285 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[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 blood coagulation factor Xa. J Med Chem. 2007 Nov 1;50(22):5339-56. [Content Brief]
[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 [Content Brief]
[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 [Content Brief]
[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 [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.1763 mL | 10.8814 mL | 21.7628 mL | 54.4070 mL |
| 5 mM | 0.4353 mL | 2.1763 mL | 4.3526 mL | 10.8814 mL | |
| 10 mM | 0.2176 mL | 1.0881 mL | 2.1763 mL | 5.4407 mL | |
| 15 mM | 0.1451 mL | 0.7254 mL | 1.4509 mL | 3.6271 mL | |
| 20 mM | 0.1088 mL | 0.5441 mL | 1.0881 mL | 2.7203 mL | |
| 25 mM | 0.0871 mL | 0.4353 mL | 0.8705 mL | 2.1763 mL | |
| 30 mM | 0.0725 mL | 0.3627 mL | 0.7254 mL | 1.8136 mL | |
| 40 mM | 0.0544 mL | 0.2720 mL | 0.5441 mL | 1.3602 mL | |
| 50 mM | 0.0435 mL | 0.2176 mL | 0.4353 mL | 1.0881 mL | |
| 60 mM | 0.0363 mL | 0.1814 mL | 0.3627 mL | 0.9068 mL | |
| 80 mM | 0.0272 mL | 0.1360 mL | 0.2720 mL | 0.6801 mL | |
| 100 mM | 0.0218 mL | 0.1088 mL | 0.2176 mL | 0.5441 mL |
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