货号:A147735 同义名: Ubenimex;NK 421
Bestatin is a competitive and specific inhibitor of leucine aminopeptidase, aminopeptidase B, and triamino peptidase.
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描述 | 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[1]. |
作用机制 | Bestatin is a potent aminopeptidase inhibitor. It competes with the substrates via binding to the catalytic site of the enzyme[3]. |
Dose | Rat: 0.02 mg/kg, 2 mg/kg[3] (i.c.v.); 0.2 mg/kg, 1 mg/kg[3] (i.p.), 2.5 mg/kg - 30 mg/kg[4] (i.p.) Mice: 100 mg/kg, 200 mg/kg[1] (p.o.) |
Administration | i.c.v., i.p., p.o. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT01944176 | COPD | Phase 3 | Completed | - | Thailand ... 展开 >> Faculty of Medicine Siriraj Hospital, Mahidol University Bangkok-noi, BKK, Thailand, 10700 收起 << |
NCT03402204 | Ischemic Stroke | Phase 3 | Completed | - | - |
NCT02664558 | Pulmonary Arterial Hypertensio... 展开 >>n 收起 << | Phase 2 | Completed | - | - |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.24mL 0.65mL 0.32mL |
16.21mL 3.24mL 1.62mL |
32.43mL 6.49mL 3.24mL |
CAS号 | 58970-76-6 |
分子式 | C16H24N2O4 |
分子量 | 308.373 |
别名 | Ubenimex;NK 421;NSC 265489 |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 7 mg/mL(22.7 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 |
动物实验配方 |