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Bestatin

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Chemical Structure| 58970-76-6 同义名 : Ubenimex;NK 421;NSC 265489
CAS号 : 58970-76-6
货号 : A147735
分子式 : C16H24N2O4
纯度 : 98%
分子量 : 308.373
MDL号 : MFCD00083262
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：
生物活性
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].
临床研究
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 - -
实验方案
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
参考文献

[1]Aozuka Y, Koizumi K, Saitoh Y, Ueda Y, Sakurai H, Saiki I. Anti-tumor angiogenesis effect of aminopeptidase inhibitor bestatin against B16-BL6 melanoma cells orthotopically implanted into syngeneic mice. Cancer Lett. 2004 Dec 8;216(1):35-42.

[2]Sekine K, Fujii H, Abe F. Induction of apoptosis by bestatin (ubenimex) in human leukemic cell lines. Leukemia. 1999 May;13(5):729-34.

[3]Scornik OA, Botbol V. Bestatin as an experimental tool in mammals. Curr Drug Metab. 2001 Mar;2(1):67-85. doi: 10.2174/1389200013338748.

[4]Evans JF, Kargman S. Bestatin inhibits covalent coupling of [3H]LTA4 to human leukocyte LTA4 hydrolase. FEBS Lett. 1992 Feb 3;297(1-2):139-42. doi: 10.1016/0014-5793(92)80345-h.