751475-53-3
751475-53-3 structure
- Name: Atopaxar
- Chemical Name: 1-(3-tert-butyl-4-methoxy-5-morpholin-4-ylphenyl)-2-(5,6-diethoxy-4-fluoro-3-imino-1H-isoindol-2-yl)ethanone
- CAS Number: 751475-53-3
- Molecular Formula: C29H38FN3O5
- Molecular Weight: 527.62800
- Catalog: Signaling Pathways GPCR/G Protein Protease-Activated Receptor (PAR)
- Create Date: 2018-12-26 11:21:20
- Modify Date: 2025-08-26 17:44:36
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Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease[1][2].
| Name | 1-(3-tert-butyl-4-methoxy-5-morpholin-4-ylphenyl)-2-(5,6-diethoxy-4-fluoro-3-imino-1H-isoindol-2-yl)ethanone |
|---|---|
| Synonyms |
Atopaxar
UNII-HTI275SD2D E-5555 |
| Description | Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease[1][2]. |
|---|---|
| Related Catalog | |
| Target |
PAR-1[1] |
| 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 IC50 of 0.019 μM[2]. Atopaxar inhibits human platelet aggregation induced by thrombin or TRAP in a concentration-dependent manner[2]. Atopaxar does not inhibit PRP (platelet-rich plasma) aggregation induced by ADP, U46619, collagen, and PAR-4ap, up to a concentration of 20 μM[2]. |
| In Vivo | Atopaxar (30-100 mg/kg; p.o.) prolongs the time to occlusion by 1.8-fold and 2.4-fold, respectively, compared with controls[2]. Atopaxar does not prolong bleeding time in guinea pigs at the highest tested dosage of 1000 mg/kg[2]. Animal Model: Guinea pigs, photo-chemically-induced thrombosis (PIT) model[2] Dosage: Oral administration Administration: 10 mg/kg, 30 mg/kg, 100 mg/kg Result: At 30 and 100 mg/kg prolonged the time to occlusion by 1.8-fold and 2.4-fold, respectively, compared with controls. |
| References |
| Molecular Formula | C29H38FN3O5 |
|---|---|
| Molecular Weight | 527.62800 |
| Exact Mass | 527.28000 |
| PSA | 84.32000 |
| LogP | 4.89230 |