阿托帕沙
| 中文名称 | 阿托帕沙 |
|---|---|
| 中文同义词 | 阿托帕沙;2-(5,6-二乙氧基-7-氟-1,3-二氢-1-亚氨基-2H-异吲哚-2-基)-1-[3-(1,1-二甲基乙基)-4-甲氧基-5-(4-吗啉)苯基]乙酮;2-(5,6-二乙氧基-7-氟-1,3-二氢-1-亚氨基-2H-异吲哚-2-基)-1-[3-叔丁基-4-甲氧基-5-(4-吗啉基)苯基]乙酮 |
| 英文名称 | Atopaxar |
| 英文同义词 | 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;E555;1-(3-(tert-Butyl)-4-methoxy-5-morpholinophenyl)-2-(5,6-diethoxy-7-fluoro-1-iminoisoindolin-2-yl)ethanone;(943239-67-6) atopaxar |
| CAS号 | 751475-53-3 |
| 分子式 | C29H38FN3O5 |
| 分子量 | 527.63 |
| EINECS号 | |
| 相关类别 | 小分子抑制剂;小分子抑制剂，天然产物;Inhibitors |
| Mol文件 | 751475-53-3.mol |
| 结构式 |  |
阿托帕沙 性质
| 沸点 | 671.0±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.22 |
| 储存条件 | Store at -20°C |
| 溶解度 | DMSO：250 mg/mL（473.82 mM；需要超声波） |
| 酸度系数(pKa) | 7.43±0.20(Predicted) |
PAR-1
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.
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.
Atopaxar (30-100 mg/kg; p.o.) 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 |
| 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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-18200 | Atopaxar | 1 mg | 685元 | |
| 2024/01/25 | HY-18200 | 2-(5,6-二乙氧基-7-氟-1,3-二氢-1-亚氨基-2H-异吲哚-2-基)-1-[3-叔丁基-4-甲氧基-5-(4-吗啉基)苯基]乙酮 Atopaxar | 751475-53-3 | 5mg | 1800元 |