|
|
| | Atopaxar Basic information |
| Product Name: | Atopaxar | | Synonyms: | 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;(943239-67-6) atopaxar | | CAS: | 751475-53-3 | | MF: | C29H38FN3O5 | | MW: | 527.63 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 751475-53-3.mol |  |
| | Atopaxar Chemical Properties |
| 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) |
| | Atopaxar Usage And Synthesis |
| 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.
| Animal Model: | Guinea pigs, PIT model | | Dosage: | Oral administration | | Administration: | 10 mg/kg, 30 mg/kg, 100 mg/kg | < td class="col1 fwb"> Result: | 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 | |
| | Atopaxar Preparation Products And Raw materials |
|