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
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
N-Bromosuccinimide Price
- Product number
- SML3064
- Product name
- Atopaxar hydrobromide
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $179
- Updated
- 2024/03/01
- Product number
- SML3064
- Product name
- Atopaxar hydrobromide
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $576
- Updated
- 2024/03/01
- Product number
- DC9198
- Product name
- Atopaxar(E5555)
- Purity
- >98%
- Packaging
- 100mg
- Price
- $750
- Updated
- 2021/12/16
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.
| 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
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