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751475-53-3

中文名稱 2-(5,6-二乙氧基-7-氟-1,3-二氫-1-亞氨基-2H-異吲哚-2-基)-1-[3-叔丁基-4-甲氧基-5-(4-嗎啉基)苯基]乙酮
英文名稱 ER 172594-00
CAS 751475-53-3
分子式 C29H38FN3O5
分子量 527.63
MOL 文件 751475-53-3.mol
更新日期 2024/12/23 09:09:17
751475-53-3 結(jié)構(gòu)式 751475-53-3 結(jié)構(gòu)式

基本信息

中文別名
阿托帕沙
2-(5,6-二乙氧基-7-氟-1,3-二氫-1-亞氨基-2H-異吲哚-2-基)-1-[3-叔丁基-4-甲氧基-5-(4-嗎啉基)苯基]乙酮
2-(5,6-二乙氧基-7-氟-1,3-二氫-1-亞氨基-2H-異吲哚-2-基)-1-[3-(1,1-二甲基乙基)-4-甲氧基-5-(4-嗎啉)苯基]乙酮
英文別名
E555
CS-666
E 5555
Atopaxa
Atopaxar
ER 172594-00
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
1-(3-tert-butyl-4-Methoxy-5-Morpholino-phenyl)-2-(5,6-diethoxy-7-fluoro-1-iMino-1,3-dihydro-isoindol-2-yl)-ethanone
所屬類別
生物化工:激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

沸點(diǎn)671.0±65.0 °C(Predicted)
密度1.22
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO : 250 mg/mL (473.82 mM; Need ultrasonic)
酸度系數(shù)(pKa)7.43±0.20(Predicted)
形態(tài)Solid
顏色White to off-white

常見(jiàn)問(wèn)題列表

生物活性
Atopaxar (E5555) 是一種高效、有口服活性活性的,選擇性的,可逆的凝血酶受體蛋白酶激活受體-1 (PAR-1) 拮抗劑。Atopaxar 能干擾血小板信號(hào)。Atopaxar 可用于動(dòng)脈粥樣硬化血栓性疾病的研究。
靶點(diǎn)

PAR-1

體外研究

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.

體內(nèi)研究

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.
"751475-53-3" 相關(guān)產(chǎn)品信息
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