Art. -Nr.: HY-50667

Apixaban

(Synonyms: BMS-562247-01)

13 Cited Publications

Kundenbewertung

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 K_i 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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Reinheit: 99.99%
CAS. Nr.: 503612-47-3
Formel: C₂₅H₂₅N₅O₄
Molecular Weight:459.50

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Apixaban Chemical Structure

CAS. Nr.: 503612-47-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (13)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Apixaban (BMS-562247-01) is a highly selective, reversible and orally active inhibitor of Factor Xa with K_i of 0.08 nM and 0.17 nM in human and rabbit, respectively^[1]. Apixaban is in development for the prevention and treatment of various thromboembolic diseases^[2].

IC₅₀ & Target

IC50: 0.08 nM (Human Factor Xa), 0.17 nM (Rabbit Factor Xa)

Cellular Effect

Cell Line	Type	Value	Description	References
Caco-2	CC₅₀	18.07 μM Compound: APIXABAN	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	10.21203/rs.3.rs-23951/v1
Caco-2	IC₅₀	5.91 μM Compound: APIXABAN	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	10.21203/rs.3.rs-23951/v1
Platelet	EC₅₀	0.07 μM Compound: Apixaban	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	[PMID: 36462436]

In Vitro

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 Vivo

Apixaban (BMS-562247-01) shows the excellent pharmacokinetics with very low clearance (Cl: 0.02 L/kg/h), and low volume of distribution (Vdss: 0.2 L/kg) in the dogs. 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), 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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 503612-47-3
Appearance Solid
Molecular Weight 459.50
Formel C₂₅H₂₅N₅O₄
Color White to off-white
SMILES

NC(C1=NN(C2=C1CCN(C2=O)C3=CC=C(C=C3)N4CCCCC4=O)C5=CC=C(C=C5)OC)=O
Synonyms

BMS-562247-01
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (13)

All In Vivo ImagingBio/Physico-chemical AssayOthers

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Journal Impact Factor

Nature

2026 Jun 24. PMID: 42343133
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

Non-classical neutrophil extracellular traps induced by PAR2-signaling proteases. [Abstract]

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.
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

Role of the activation peptide in the mechanism of protein C activation. [Abstract]

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.
J Chem Thermodyn

2020 May.
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.
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.
LabMed

2024 Nov 18.
Elife

Coagulation factors directly cleave SARS-CoV-2 spike and enhance viral entry. [Abstract]

2022 Mar 23:11:e77444. PMID: 35294338
Personalized Medicine Universe

2019 May.
Patent

US20170224812A1.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

Kinase Assay^[2]

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 (K_m), 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 K_i 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.

Animal Administration^[2]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (393 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
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

Keywords

Apixaban

13 Cited Publications

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Apixaban

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Publications Citing Use of MedChemExpress (MCE) Apixaban

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Apixaban Related Classifications

HY-50667 Related Classifications