1. Metabolic Enzyme/Protease Anti-infection
  2. Proteasome Parasite
  3. Antitrypanosomal agent 15

Antitrypanosomal agent 15 (compound 26) 是一种口服有效、脑渗透、选择性的克氏锥虫蛋白酶体 (Trypanosoma cruzi proteasome) 抑制剂,对克氏锥虫和人蛋白酶体的 pIC50 分别为 7.4 和 <4。Antitrypanosomal agent 15 具有良好的ADME特性,可用于恰加斯病的研究。

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Antitrypanosomal agent 15 Chemical Structure

Antitrypanosomal agent 15 Chemical Structure

CAS No. : 2961381-94-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

体外研究
(In Vitro)

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[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

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[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: The chronic mouse model of Chagas disease[1]
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.
分子量

410.40

Formula

C21H19FN4O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Antitrypanosomal agent 15
目录号:
HY-155103
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