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Bestatin

氨肽酶抑制剂，Bestatin是一种天然，广谱，竞争性的氨肽酶抑制剂。

目录号: PC15611 纯度: ≥98%

CAS No. :58970-76-6

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中文名称	Bestatin
中文别名	乌苯美司;N-[(2S,3R)-3-氨基-2-羟基-4-苯丁酰]-L-亮氨酸;贝他定;贝他定(苯丁抑制素);乌苯美司(乌苯美司);乌苯美司-D5(乌苯美司-D5);乌苯美司-D7(乌苯美司-D7);乌苯美司对照品;乌苯美司及其中间体;抑氨肽酶;抑氨肽酶,乌苯美司,贝他定;([2S,3R]-3-氨基-2-羟基-4-苯基丁酰基)-L-亮氨酸;[S-(R,S)]-N-(3-氨基-2-羟基-1-氧代-4-苯丁基)-L-亮氨酸;N -[（2S,3R）-3 -氨基- 2-羟基- 4-苯基丁酰] -L 亮氨酸;N-[(2S,3R)-3-氨基-2-羟基-4-苯基丁酰基]-L-亮氨酸;乌苯美司,N-[(2S,3R)-3-氨基-2-羟基-4-苯基丁酰基]-L-亮氨酸
英文名称	Bestatin
英文别名	ubenimex;(S)-2-((2S,3R)-3-Amino-2-hydroxy-4-phenylbutanamido)-4-methylpentanoic acid;[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutyryl]-L-leucine;[(2S003R)-3-Amino-2-hydroxy-4-phenylbutyryl]-L-leucine;BESTATIN;N-((2S,3R)-3-AMINO-2-HYDROXY-4-PHENYLBUTYRYL)-L-LEUCINE;N-[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutyryl]-L-leucine;BENIMEX;Bestatin,UbeniMex;nk421;[S-(R,S)]-N-(3-Amino-2-hydroxy-1-oxo-4-phenylbuty1)-L-leucine;Direnavir;Bestatin;Ubenimex;Ubenimexum [Latin];Ubenimex (Bestatin);Ubenimex [INN:JAN];Ubenimex(Bestatin);NK 421;I0J33N5627;3-(R)-Amino-2-(S)-hydroxy-4-phenylbutanoyl-(S)-leucine;[(2s,3r)-3-amino-2-hydroxy-4-phenylbutanoyl]-l-leucine;N-[(2S,3R)-3-Amino-2-hydroxy-4
Cas No.	58970-76-6
分子式	C₁₆H₂₄N₂O₄
分子量	308.37
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Bestatin is a natural, broad-spectrum, and competitive CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase inhibitor. Bestatin has anticancer effects.

性状

Solid

IC50 & Target[1][2]

CD13

体外研究(In Vitro)

Bestatin enhances ATRA-induced differentiation and inhibits ATRA-driven phosphorylation of p38 MAPK in ATRA-sensitive APL NB4 cells. Bestatin can not reverse the differentiation block in ATRA-resistant APL MR2 cells. CD13 ligation with anti-CD13 antibody WM-15 results in phosphorylation of p38 MAPK, reduces the inhibition of Bestatin on the phosphorylation of p38 MAPK, and completely abolishes the enhancement of Bestatin on ATRA-inducing differentiation in NB4 cells. Bestatin (600 μM)-treated cells progress slower through the cell cycle due to decreased rate of cell growth and the frequency of cell division. Bestatin inhibits the frequency of mitosis and the inherent multinuclearity in D. discoideum, and is not cytotoxic to D. discoideum cells at 0-600 μM. Bestatin inhibits aminopeptidase activity in lysates of PsaA-GFP- and GFP-expressing cells by 69.39% and 39.93% of control, respectively.

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

体内研究(In Vivo)

Bestatin (20 μM) significantly reduces CD13 expression in diabetic mice and results a significant inhibition of MMP-9 specific gelationolytic band densities compared to diabetic vehicle-treated mice. Bestatin treatment significantly inhibits the expression of VEGF and heparanase in diabetic mice. Intravitreal bestatin treatment significantly downregulates the expression of both HIF-1α and VEGF in diabetic mice retinas. Furthermore, the upregulated expression of heparanase in diabetic mice retinas is significantly inhibited by intravitreal bestatin treatment. Bestatin (10, 1, and 0.1mg/kg, i.p.) treatment before the antigen-potentiated humoral response to SRBC results in an increased number of splenocytes producing hemolytic anti-SRBC antibodies (PFC) and the 2-ME-resistant serum hemagglutinin titer (at a dose of 0.1 mg/kg). Bestatin (1 and 0.1 mg/kg) administered to mice five times on alternate days after cyclophosphamide injection does not change the suppressive effect of the drug regarding the number of PFC, and even causes the further decrease of the total anti-SRBC hemagglutinins at dose of 1 mg/kg on day 7 after antigen stimulation.

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

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

结构分类

Ketones, Aldehydes, Acids

来源

Streptomyces olivoreticuli

参考文献

[1]. Hossain A, et al. Protective effects of bestatin in the retina of streptozotocin-induced diabetic mice. Exp Eye Res. 2016 Aug;149:100-6 [Information]

[2]. Qian X, et al. Inhibition of p38 MAPK Phosphorylation Is Critical for Bestatin to Enhance ATRA-Induced Cell Differentiation in Acute Promyelocytic Leukemia NB4 Cells. Am J Ther. 2016 May-Jun;23(3):e680-9. [Information]

[3]. Lis M, et al. The effects of bestatin on humoral response to sheep erythrocytes in non-treated and cyclophosphamide-immunocompromised mice. Immunopharmacol Immunotoxicol. 2013 Feb;35(1):133-8 [Information]

[4]. Poloz Y, et al. Bestatin inhibits cell growth, cell division, and spore cell differentiation in Dictyostelium discoideum. Eukaryot Cell. 2012 Apr;11(4):545-57 [Information]

溶解度数据

体外研究:

DMSO : 8.33 mg/mL (27.01 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2429 mL	16.2143 mL	32.4286 mL
5 mM	0.6486 mL	3.2429 mL	6.4857 mL
10 mM	0.3243 mL	1.6214 mL	3.2429 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 0.83 mg/mL (2.69 mM); Clear solution

此方案可获得 ≥ 0.83 mg/mL (2.69 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 0.83 mg/mL (2.69 mM); Clear solution

此方案可获得 ≥ 0.83 mg/mL (2.69 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 0.83 mg/mL (2.69 mM); Clear solution

此方案可获得 ≥ 0.83 mg/mL (2.69 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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