| Identification | Back Directory | [Name]
ER 172594-00 | [CAS]
751475-53-3 | [Synonyms]
E555
E 5555
CS-666
Atopaxa
Atopaxar
ER 172594-00
Atopaxar (E 5555)
(943239-67-6) atopaxar
1-(3-(tert-Butyl)-4-methoxy-5-morpholinophenyl)-2-(5,6-diethoxy-7-fluoro-1-iminoisoindolin-2-yl)ethanone
1-(3-tert-butyl-4-Methoxy-5-Morpholino-phenyl)-2-(5,6-diethoxy-7-fluoro-1-iMino-1,3-dihydro-isoindol-2-yl)-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]ethanone
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]- | [Molecular Formula]
C29H38FN3O5 | [MDL Number]
MFCD20040417 | [MOL File]
751475-53-3.mol | [Molecular Weight]
527.63 |
| Chemical Properties | Back Directory | [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) | [form ]
Solid | [pka]
7.43±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [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]
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| Company Name: |
DebyeTec.com Inc.
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| Tel: |
18086626237 18086626237 |
| Website: |
https://www.debyetec.com |
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