货号:A459084 同义名: 盐酸乌苯美司 / Ubenimex hydrochloride;Bestatin (hydrochloride)
Bestatin HCl is a competitive and specific inhibitor of leucine aminopeptidase, aminopeptidase B, and triamino peptidase.
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描述 | Bestatin Hydrochloride is a hydrochloride form of Bestatin. Bestatin is a potent inhibitor of aminopeptidases. The Ki 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]. |
Dose | 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.) |
Administration | i.p., p.o. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.90mL 0.58mL 0.29mL |
14.50mL 2.90mL 1.45mL |
29.00mL 5.80mL 2.90mL |
CAS号 | 65391-42-6 |
分子式 | C16H25ClN2O4 |
分子量 | 344.834 |
别名 | 盐酸乌苯美司 ;Ubenimex hydrochloride;Bestatin (hydrochloride);Bestatin hydrochloride |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 250 mg/mL(724.99 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 100 mg/mL(289.99 mM),配合低频超声助溶 |
动物实验配方 |