Atopaxar
Atopaxar Basic information
- Product Name:
- Atopaxar
- Synonyms:
-
- (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
- CAS:
- 751475-53-3
- MF:
- C29H38FN3O5
- MW:
- 527.63
- 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)
- form
- Solid
- color
- White to off-white
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 |
| 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
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