阿托帕沙
|
|
|
- CAS号:
- 751475-53-3
- 英文名:
- Atopaxar
- 英文别名:
- 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
- 中文名:
- 阿托帕沙
- 中文别名:
- 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-叔丁基-4-甲氧基-5-(4-吗啉基)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-(1,1-二甲基乙基)-4-甲氧基-5-(4-吗啉)苯基]乙酮
- CBNumber:
- CB52521159
- 分子式:
- C29H38FN3O5
- 分子量:
- 527.63
- MOL File:
- 751475-53-3.mol
|
|
|
阿托帕沙化学性质
-
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; Need ultrasonic)
-
|
-
酸度系数(pKa):
-
7.43±0.20(Predicted)
-
|
阿托帕沙性质、用途与生产工艺
Atopaxar (E5555) 是一种高效、有口服活性活性的，选择性的，可逆的凝血酶受体蛋白酶激活受体-1 (PAR-1) 拮抗剂。Atopaxar 能干扰血小板信号。Atopaxar 可用于动脉粥样硬化血栓性疾病的研究。
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.
|
阿托帕沙
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 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 |
751475-53-3, 阿托帕沙 相关搜索:
- Inhibitors
- 合成有机化合物配体
- 小分子抑制剂，天然产物
- 小分子抑制剂
- C29H38FN3O5
- 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
- 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
- 阿托帕沙
- 751475-53-3
- E5555,platelets,Atopaxar,receptor-1,signaling,PAR-1,inhibit,E-5555,Inhibitor,receptor,Protease Activated Receptor (PAR),protease-activated,atherothrombotic,E 5555,thrombin,Thrombin receptors
- Benzoicacid,4-hydroxy-3,6-dimethoxy-
- Ethanone, 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]-
- Atopaxa
- CS-666
- Atopaxar (E 5555)
- (943239-67-6) atopaxar
- 1-(3-(tert-Butyl)-4-methoxy-5-morpholinophenyl)-2-(5,6-diethoxy-7-fluoro-1-iminoisoindolin-2-yl)ethanone
- E555
- 1-(3-tert-butyl-4-Methoxy-5-Morpholino-phenyl)-2-(5,6-diethoxy-7-fluoro-1-iMino-1,3-dihydro-isoindol-2-yl)-ethanone
- E 5555
- Atopaxar
- 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
- ER 172594-00