1. Metabolic Enzyme/Protease
  2. MetAP
  3. NS-181

NS-181 是一种具有口服活性的 MetAP2 抑制剂和抗阿米巴剂。NS-181 可在功能上抑制甲硫氨酸氨基肽酶 2,该蛋白是 Entamoeba histolytica (溶组织内阿米巴) 增殖的关键蛋白。NS-181 对 Entamoeba histolytica 具有抗阿米巴活性,可使阿米巴肝脓肿消退。NS-181 可用于阿米巴病的研究。

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NS-181

NS-181 Chemical Structure

CAS No. : 3075693-63-6

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生物活性

NS-181 is a MetAP2 inhibitor and antiamebic agent with oral effectiveness.NS-181 functionally inhibits methionine aminopeptidase 2, a protein critical for Entamoeba histolytica proliferation. NS-181 exerts antiamebic activity against Entamoeba histolytica, leading to resolution of amebic liver abscess. NS-181 can be used for the research of amebiasis[1].

体外研究
(In Vitro)

NS-181 (30 min) 可抵抗仓鼠肝微粒体介导的代谢,且在微粒体孵育 30 分钟后仍保留强效抗阿米巴活性 (ED50 of 14.6 nM)[1]
NS-181 (10 μM) 对人肝癌细胞 Huh-7 无细胞毒性[1]

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

体内研究
(In Vivo)

NS-181 (15-30 mg/kg; s.c., p.o.; 5 consecutive days) 在仓鼠中,15 mg/kg 皮下给药可实现阿米巴肝脓肿的完全消退,30 mg/kg 口服给药则可显著缩小脓肿大小[1]

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

Animal Model: unstated specific strain[1]
Dosage: 15 mg/kg (subcutaneous); 30 mg/kg (oral)
Administration: s.c.; 5 consecutive days; p.o.; 5 consecutive days
Result: Achieved complete resolution of amebic liver abscess, with abscess weight proportion relative to whole liver reduced to near 0%, amebic mRNA levels in liver reduced, and inflammation levels decreased to match noninfected controls.
Significantly reduced amebic liver abscess size, with abscess weight proportion relative to whole liver markedly decreased compared to vehicle controls.
分子量

428.47

Formula

C24H28O7

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:
NS-181
目录号:
HY-181644
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