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编 号：F762653
分子式：C21H19FN4O4
分子量：410.4
分子式：C21H19FN4O4
分子量：410.4
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CAS No: 2961381-94-0
产品详情
生物活性：
Antitrypanosomal agent 15 (compound 26) is an orally active, brain-penetrant, selective inhibitor against Trypanosoma cruzi proteasome, with an pIC50 of 7.4 and <4 for T. cruzi and human proteasome, respectively. Antitrypanosomal agent 15 has favorable ADME properties and can be used for Chagas disease study.
体内研究：
Antitrypanosomal agent 15 (compound 26) (50 mg/kg, 每日两次, 20 天, 口服) 显示出良好的溶解性和渗透性，但对慢性恰加斯病小鼠模型无作用。Animal Model:The chronic mouse model of Chagas disease
Dosage:50 mg/kg b.i.d for 20days
Administration:Oral gavage (p.o.)
Result:Was not curative . Was above EC99 for approximately 5 h after the first dose on day 1, but dropped to less than 2 h after the first dose by day 20.
体外研究：
Antitrypanosomal agent 15 (compound 26) 对T. cruzi amastigotes和宿主 VERO 细胞的pEC50 分别为 6.1 和 4.4，外排比为 1.8，FaSSIF (空腹模拟肠液溶解度) 为 339 μM。
Antitrypanosomal agent 15 (compound 26) is an orally active, brain-penetrant, selective inhibitor against Trypanosoma cruzi proteasome, with an pIC50 of 7.4 and <4 for T. cruzi and human proteasome, respectively. Antitrypanosomal agent 15 has favorable ADME properties and can be used for Chagas disease study.
体内研究：
Antitrypanosomal agent 15 (compound 26) (50 mg/kg, 每日两次, 20 天, 口服) 显示出良好的溶解性和渗透性，但对慢性恰加斯病小鼠模型无作用。Animal Model:The chronic mouse model of Chagas disease
Dosage:50 mg/kg b.i.d for 20days
Administration:Oral gavage (p.o.)
Result:Was not curative . Was above EC99 for approximately 5 h after the first dose on day 1, but dropped to less than 2 h after the first dose by day 20.
体外研究：
Antitrypanosomal agent 15 (compound 26) 对T. cruzi amastigotes和宿主 VERO 细胞的pEC50 分别为 6.1 和 4.4，外排比为 1.8，FaSSIF (空腹模拟肠液溶解度) 为 339 μM。
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