ChemicalBook > CAS DataBase List > Atopaxar

Atopaxar

Product Name
Atopaxar
CAS No.
751475-53-3
Chemical Name
Atopaxar
Synonyms
E555;CS-666;E 5555;Atopaxa;Atopaxar;ER 172594-00;Atopaxar (E 5555);(943239-67-6) atopaxar;Benzoicacid,4-hydroxy-3,6-dimethoxy-;1-(3-(tert-Butyl)-4-methoxy-5-morpholinophenyl)-2-(5,6-diethoxy-7-fluoro-1-iminoisoindolin-2-yl)ethanone
CBNumber
CB52521159
Molecular Formula
C29H38FN3O5
Formula Weight
527.63
MOL File
751475-53-3.mol
More
Less

Atopaxar Property

Boiling point:
671.0±65.0 °C(Predicted)
Density 
1.22
storage temp. 
Store at -20°C
solubility 
DMSO : 250 mg/mL (473.82 mM; Need ultrasonic)
pka
7.43±0.20(Predicted)
form 
Solid
color 
White to off-white
More
Less

Hazard and Precautionary Statements (GHS)

More
Less

N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML3064
Product name
Atopaxar hydrobromide
Purity
≥98% (HPLC)
Packaging
5MG
Price
$179
Updated
2024/03/01
Sigma-Aldrich
Product number
SML3064
Product name
Atopaxar hydrobromide
Purity
≥98% (HPLC)
Packaging
25MG
Price
$576
Updated
2024/03/01
DC Chemicals
Product number
DC9198
Product name
Atopaxar(E5555)
Purity
>98%
Packaging
100mg
Price
$750
Updated
2021/12/16
More
Less

Atopaxar Chemical Properties,Usage,Production

Definition

ChEBI: Atopaxar is an aromatic ketone.

Biological Activity

Atopaxar (E5555) is a potent, orally active, selective, reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. It can be used in the study of atherothrombotic diseases and interferes with platelet signaling..

in vitro

Atopaxar inhibits haTRAP (high-affinity thrombin receptor activating peptide) binding to PAR-1 on human platelet membranes in a concentration-dependent manner, with an IC 50 of 0.019 μM. < br/> Atopaxar inhibits human platelet aggregation induced by thrombin or TRAP in a concentration-dependent manner.
Atopaxar does not inhibit PRP (platelet-rich plasma) aggregation induced by ADP, U46619, collagen, and PAR-4ap, up to a concentration of 20 μM.

in vivo

Atopaxar (30-100 mg/kg; po) causes a dose-dependent prolongation of the time to occlusion of the femoral artery in photochemically-induced thrombosis (PIT) guinea pigs model.
Atopaxar does not prolong bleeding time in guinea pigs at the highest tested dosage of 1000 mg/kg.

< td class="col1 fwb"> Result:
Animal Model: Guinea pigs, PIT model
Dosage: Oral administration
Administration: 10 mg/kg, 30 mg/kg, 100 mg/kg
Prolonged the time to occlusion by 1.8-fold and 2.4-fold at 30 mg/kg and 100 mg/kg, respectively, compared with controls.

target

PAR-1

Atopaxar Preparation Products And Raw materials

Raw materials

Preparation Products

More
Less

Atopaxar Suppliers

Axon Medchem BV
Tel
--
Fax
--
Email
info@axonmedchem.com
Country
The Netherlands
ProdList
477
Advantage
30

751475-53-3, AtopaxarRelated Search:


  • (943239-67-6) atopaxar
  • Atopaxar (E 5555)
  • CS-666
  • ER 172594-00
  • 2-(5,6-Diethoxy-7-fluoro-1,3-dihydro-1-imino-2H-isoindol-2-yl)-1-[3-(1,1-dimethylethyl)-4-methoxy-5-(4-morpholinyl)phenyl]ethanone
  • Atopaxar
  • E 5555
  • 1-(3-tert-butyl-4-Methoxy-5-Morpholino-phenyl)-2-(5,6-diethoxy-7-fluoro-1-iMino-1,3-dihydro-isoindol-2-yl)-ethanone
  • E555
  • 1-(3-(tert-Butyl)-4-methoxy-5-morpholinophenyl)-2-(5,6-diethoxy-7-fluoro-1-iminoisoindolin-2-yl)ethanone
  • Atopaxa
  • Ethanone, 2-(5,6-diethoxy-7-fluoro-1,3-dihydro-1-imino-2H-isoindol-2-yl)-1-[3-(1,1-dimethylethyl)-4-methoxy-5-(4-morpholinyl)phenyl]-
  • Benzoicacid,4-hydroxy-3,6-dimethoxy-
  • E5555,platelets,Atopaxar,receptor-1,signaling,PAR-1,inhibit,E-5555,Inhibitor,receptor,Protease Activated Receptor (PAR),protease-activated,atherothrombotic,E 5555,thrombin,Thrombin receptors
  • 751475-53-3
  • C29H38FN3O5
  • Inhibitors