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产品编号:  AD.Y00015-1g 中文名称:  乌苯美司
中文别名:  N-[(2S,3R)-3-氨基-2-羟基-4-苯基丁酰基]-L-亮氨酸 英文名称:  ubeniMex
英文别名:  BESTATIN 品牌: ANDY
规格型号:  1g CAS号:  58970-76-6
分子式:  C16H24N2O4 分子量: 308.37
外观与性状:  白色结晶粉末 储存条件: 2-8°C
纯度:  99.5%
标准价:  250.00 优惠价:   登录查看
数量:  

单位:  
库存与货期:  订货

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商品信息

生物活性

Bestatin is a natural, broad-spectrum, and competitive aminopeptidase inhibitor.

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[2]. 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[4].

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[1]. 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[3].

Clinical Trial

NCT Number

Sponsor

Condition

Start Date

Phase

NCT02664558

Eiger BioPharmaceuticals

Pulmonary Arterial Hypertension

April 2016

Phase 2

NCT02736149

Eiger BioPharmaceuticals

Pulmonary Arterial Hypertension

December 2016

Phase 2

NCT02700529

Eiger BioPharmaceuticals

Lymphedema

June 2016

Phase 2

分子量

308.37

Formula

C??H??N?O?

CAS

58970-76-6

中文名称

乌苯美司

SMILES

CC(C)C[C@@H](C(O)=O)NC([C@@H](O)[C@H](N)CC1=CC=CC=C1)=O

运输条件

Room temperature in continental US; may vary elsewhere.

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)

溶解性数据

In Vitro: 

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

配制储备液

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

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,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,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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.

请依序添加每种溶剂: 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。

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

  • 2.

请依序添加每种溶剂: 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。

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% SBE-β-CD 生理盐水水溶液中,混合均匀。

  • 3.

请依序添加每种溶剂: 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。

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。

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

[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.

[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

[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


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