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CAS No.: 65391-42-6

Bestatin HCl/乌苯美司盐酸盐 Catalog No. CSN10420

Synonyms: Ubenimex hydrochloride;Ubenimex HCl;Bestatin (hydrochloride)

Bestatin HCl is a competitive and specific inhibitor of leucine aminopeptidase, aminopeptidase B, and triamino peptidase.

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实验方案

技术信息

生物活性

描述Bestatin Hydrochloride is a hydrochloride form of Bestatin. Bestatin is a potent inhibitor of aminopeptidases. The K_i values for bestatin against leucyl aminopeptidase, tripeptide aminopeptidase, cytosol alanyl aminopeptidase, leukotriene A4 hydrolase, aminopeptidase B and nardilysin were 1nM, 0.5μM, 14nM, 0.17μM, 1μM and 15μM, respectively^[3]. Pre-incubation of human leukocyte LTA₄ hydrolase with 1, 10, or 100μM bestatin resulted in 20%, 50%, and 90% inhibition of [³H]LTA₄ labeling of LTA₄ hydrolase, respectively. Bestatin inhibited LTB₄ formation by LTA₄ hydrolase in a dose-dependent manner with 50% inhibition of activity at 10μM^[4]. In human umbilical vein endothelial cells (HUVECs), bestatin at 1-100mg/ml inhibited the Ala-MCA-hydrolysing activity of cells in a dose-dependent manner. Bestatin at the same concentration range also resulted in the formation of shorter branching structures in HUVECs compared to the controls. In C57BL/6 mice implanted with B16-BL6 melanoma cells into the dorsal side, intraperitoneal administration of bestatin (50 or 100 mg/kg/day) for 5 days significantly reduced the number of vessels oriented towards the tumor mass without affecting the tumor volume^[5].
作用机制Bestatin is a potent aminopeptidase inhibitor. It competes with the substrates via binding to the catalytic site of the enzyme^[6].
动物研究
剂量
Mice: 0.1 mg/kg - 10 mg/kg^[3] (i.p.), 50 mg/kg - 100 mg/kg^[4] (i.p.); 100 mg/kg - 200 mg/kg^[4] (p.o.)

给药途径
i.p., p.o.
参考文献

动物研究
剂量	Mice: 0.1 mg/kg - 10 mg/kg^[3] (i.p.), 50 mg/kg - 100 mg/kg^[4] (i.p.); 100 mg/kg - 200 mg/kg^[4] (p.o.)
给药途径	i.p., p.o.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8999 mL
- 14.4997 mL
- 28.9995 mL
- 5 mM
- 0.5800 mL
- 2.8999 mL
- 5.7999 mL
- 10 mM
- 0.2900 mL
- 1.4500 mL
- 2.8999 mL

技术信息

CAS号	65391-42-6	储存条件	粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C16H25ClN2O4	运输	蓝冰
分子量	344.83	别名	Ubenimex hydrochloride;Ubenimex HCl;Bestatin (hydrochloride);Bestatin HCl;Ubenimex;NK-421;Bestatin;NSC-265489;盐酸乌苯美司;盐酸贝他汀

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