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Bestatin hydrochloride

氨肽酶N（APN/CD13）和氨肽酶B抑制剂，Bestatin hydrochloride 是 CD13 (Aminopeptidase N)/APN 和 leukotriene A4 hydrolase 抑制剂，常用于癌症治疗。

目录号: PC15718 纯度: ≥98%

CAS No. :65391-42-6

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中文名称	Bestatin hydrochloride
中文别名	贝他定盐酸;N-[(2S,3R)-3-氨基-2-羟基-4-苯基丁酰基]-L-亮氨酸盐酸盐;氨肽酶;苯丁抑制素盐酸盐;盐酸甜菜碱,乌苯美司;盐酸乌苯美司;N-[(2S,3R)-3-氨基-2-羟基-4苯基丁]-L-亮氨酸盐酸盐;盐酸贝他定;盐酸倍他定;(-)-贝他汀盐酸盐;盐酸乌苯美司;贝他定盐酸盐;N-[(2S,3R)-3-氨基-2-羟基-4-苯丁酸]-L-亮氨酸盐酸盐
英文名称	Bestatin hydrochloride
英文别名	L-Leucine,N-[(2S,3R)-3-amino-2-hydroxy-1-oxo-4-phenylbutyl]-, hydrochloride (1:1);Ubenimex Hydrochloride [for Biochemical Research];Bestatin (hydrochloride);Bestatin hydrochloride;Ubenimex hydrochloride;Bestatin.HCI;N-[(2S,3R)-3-AMino-2-hydroxy-4-phenylbutyryl]-L-leucine Hydrochloride;N-(3-Amino-2-hydroxy-1-oxo-4-phenylbutyl)-L-leucine monohydrochloride;BESTATIN HCL;Bestatin monohydrochloride;C16H24N2O4.HCl;BIMI2137;Tox21_500214;LP00214;API0001675;Bestatin hydrochloride, >=98% (HPLC);AB0020587;V1527;B4000;M01391;B 8385;SR
Cas No.	65391-42-6
分子式	C₁₆H₂₅ClN₂O₄
分子量	344.83
包装储存	4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

生物活性

Bestatin hydrochloride is an inhibitor of CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase, used for cancer research.

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% ± 10.5% and 39.93% ± 18.7% 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, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

ClinicalTrial

结构分类

Ketones, Aldehydes, Acids

来源

Actinomycetes

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 : 250 mg/mL (724.99 mM; Need ultrasonic)

H₂O : 100 mg/mL (290.00 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	2.9000 mL	14.4999 mL	28.9998 mL
5 mM	0.5800 mL	2.9000 mL	5.8000 mL
10 mM	0.2900 mL	1.4500 mL	2.9000 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 (stored under nitrogen)。-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： PBS
Solubility: 50 mg/mL (145.00 mM); Clear solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (6.03 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.03 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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
3.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (6.03 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.03 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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
4.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (6.03 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.03 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 20.8 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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