Atopaxar
- CAS NO.：751475-53-3
- Empirical Formula: C29H38FN3O5
- Molecular Weight: 527.63
- MDL number: MFCD20040417
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-07-02 08:55:11
What is Atopaxar?
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. |
Properties of Atopaxar
| 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 |
Safety information for Atopaxar
Computed Descriptors for Atopaxar
New Products
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