Apixaban (BMS 562247-01)

Catalog No.S1593

For research use only.

Apixaban (BMS 562247-01) is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.

Apixaban (BMS 562247-01) Chemical Structure

CAS No. 503612-47-3

Selleck's Apixaban (BMS 562247-01) has been cited by 21 publications

Purity & Quality Control

Choose Selective Factor Xa Inhibitors

Other Factor Xa Products

Biological Activity

Description Apixaban (BMS 562247-01) is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.
Features A highly selective, reversible, and direct factor Xa inhibitor.
Targets
Factor Xa (human) [1]
(Cell-free assay)
Factor Xa (rabbit) [1]
(Cell-free assay)
0.08 nM(Ki) 0.17 nM(Ki)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A673 MkGxdWhVWyCjc4PhfS=> MkHxdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN? MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-37 MVLxTHRUKGG|c3H5 NXzMN5A1eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVM4KGOnbHzz NVLXU3cxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2 MkK0dWhVWyCjc4PhfS=> MljtdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2ouT0KPMjDj[Yxtew>? MmKxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh41 M3vuVJFJXFNiYYPzZZk> M3zYV5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJpPDFiY3XscJM> NXvPepQyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
RD NXHDb4JoeUiWUzDhd5NigQ>? NImyUIRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTTCClZXzsdy=> M33ORVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh30 M1S1U5FJXFNiYYPzZZk> MlPDdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgVog{OCClZXzsdy=> M1;aN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Caco-2 MXzGeY5kfGmxbjDhd5NigQ>? NXTyOnhCPDhiaILz M{\0NGRmfGW{bXnuZZRqd25ib3[gTWM2OCC4YXz1[ZMh\m:{IHnubIljcXSrb36gc4YhW0GUUz3Dc3YuOiCrbnT1Z4VlKGO7dH;0c5hq[2m2eTDv[kBE[WOxLUKgZ4VtdHNiYX\0[ZIhPDhiaH;1dpMh[nliaHnnbEBkd262ZX70JIlu[WerbnesJGlEPTB;NT65Ne69VQ>? M3f1ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI{OTd5OT:nQmNpTU2ETEyvZV4>
Caco-2 NUTE[GxtXG:6aXPpeJkh[XO|YYm= MW[0PEBpenN? M{TyfnRwgGmlaYT5JIFo[Wmwc4SgR4Fkdy1{IHPlcIx{KGSndHXycYlv\WRiYYSgOFghcG:3coOgZpkhcW62cnHj[YxtfWyjcjDBWHAh[2:wY3XueJJifGmxbjD1d4lv\yC2aHWgR4VtdFSrdHXyMWdtdyCOdX3pcoV{[2WwdDDD[YxtKF[rYXLpcIl1gSCDc4PhfUwhS0N3ME2xPE4xP87:TR?= MmSxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlMyPzd7Lze+R4hGVUKOPD;hQi=>
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]

Protocol (from reference)

Animal Research:[2]
  • Animal Models: Arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) and electrically mediated carotid arterial thrombosis (ECAT) rabbit models.
  • Dosages: ≤3 mg/kg/h
  • Administration: Administered via i.v.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 18 mg/mL
(39.17 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
30% PEG 400+0.5% Tween 80+5% Propylene glycol
For best results, use promptly after mixing.

30mg/mL

* 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.

Chemical Information

Molecular Weight 459.5
Formula

C25H25N5O4

CAS No. 503612-47-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=CC=C(C=C1)N2C3=C(CCN(C3=O)C4=CC=C(C=C4)N5CCCCC5=O)C(=N2)C(=O)N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04974684 Not yet recruiting Device: HeartMate 3|Drug: Apixaban LVAD (Left Ventricular Assist Device) Thrombosis Institute for Clinical and Experimental Medicine September 1 2021 Not Applicable
NCT03812835 Not yet recruiting -- Thrombosis Deep Vein|Pulmonary Embolism Pfizer August 23 2021 --
NCT04952792 Recruiting Drug: Apixaban 2.5 milligram Oral Tablet Atrial Fibrillation|Hemodialysis Complication Hospital Universitari de Bellvitge May 20 2021 Phase 2
NCT04278729 Recruiting Drug: Apixaban 5 MG Nephrotic Syndrome|Membranous Nephropathy University of North Carolina Chapel Hill|American College of Clinical Pharmacy April 14 2021 Phase 1
NCT04850378 Recruiting Drug: Dalteparin|Drug: Apixaban Nephrotic Syndrome|Thromboembolic Disease University of Aarhus March 25 2021 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2021-09-06)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Apixaban (BMS 562247-01) | Apixaban (BMS 562247-01) supplier | purchase Apixaban (BMS 562247-01) | Apixaban (BMS 562247-01) cost | Apixaban (BMS 562247-01) manufacturer | order Apixaban (BMS 562247-01) | Apixaban (BMS 562247-01) distributor