阿托帕沙
中文名称 | 阿托帕沙 |
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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 | (943239-67-6) atopaxar;Atopaxar (E 5555);CS-666;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 |
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) |
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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) |
形态 | 固体 |
颜色 | 白色至米白色 |
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 |
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2024/08/19 | HY-18200 | Atopaxar | 1 mg | 685元 | |
2024/08/19 | 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 |