| 中文名称: | 盐酸乌苯美司 | ||||
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| 英文名称: | Bestatin hydrochloride | ||||
| 别名: | 盐酸乌苯美司 Ubenimex hydrochloride | ||||
| CAS No: | 65391-42-6 | 分子式: | C16H25ClN2O4 | 分子量: | 344.83 |
| CAS No: | 65391-42-6 | ||||
| 分子式: | C16H25ClN2O4 | ||||
| 分子量: | 344.83 | ||||
基本信息
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产品编号： |
B10559 |
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产品名称： |
Bestatin hydrochloride |
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CAS: |
65391-42-6 |
储存条件 |
粉末 |
2-8℃充氮保存 |
三年 |
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分子式： |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
344.83 |
-20℃ |
一个月 |
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化学名： |
(S)-2-((2S,3R)-3-amino-2-hydroxy-4-phenylbutanamido)-4-methylpentanoic acid hydrochloride |
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Solubility (25°C)： |
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体外:
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DMSO |
250mg/mL(724.99mM;Need ultrasonic) |
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Ethanol |
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Water |
100mg/mL(290.00mM;Need ultrasonic) |
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体内(现配现用): |
1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility:≥2.08mg/mL(6.03mM);Clear solution |
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此⽅案可获得≥2.08mg/mL(6.03mM，饱和度未知)的澄清溶液。以1mL⼯作液为例，取100μL20.8mg/mL的澄清DMSO储备液加到400μL PEG300中，混合均匀；向上述体系中加⼊50μL Tween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。 |
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2.请依序添加每种溶剂：10% DMSO→90% (20% SBE-β-CD in saline) Solubility:≥2.08mg/mL(6.03mM);Clear solution |
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此⽅案可获得≥2.08mg/mL(6.03mM，饱和度未知)的澄清溶液。以1mL⼯作液为例，取100μL20.8mg/mL的澄清DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶液中，混合均匀。 |
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3.请依序添加每种溶剂：10% DMSO→90% corn oil Solubility:≥2.08mg/mL(6.03mM);Clear solution |
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此⽅案可获得≥2.08mg/mL(6.03mM，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1mL⼯作液为例，取100μL20.8mg/mL的澄清DMSO储备液加到900μL⽟⽶油中，混合均匀。 |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.9000mL |
14.4999mL |
28.9998mL |
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5mM |
0.5800mL |
2.9000mL |
5.8000mL |
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10mM |
0.2900mL |
1.4500mL |
2.9000mL |
生物活性
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产品描述 |
一种CD13 (Aminopeptidase N)/APN 和 leukotriene A4 hydrolase 抑制剂。 |
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靶点 |
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体外研究 |
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 antiCD13 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 (600μM)-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 0-600μM. 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 |
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体内研究 |
Bestatin (20μM) significantly reduces CD13 expression in diabetic mice and results a significant inhibition ofmMP-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 0.1mg/kg). Bestatin (1 and 0.1mg/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 1mg/kg on day 7 after antigen stimulation |
推荐实验方法(仅供参考)
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Kinase Assay |
Cells are harvested, washed, and lysed in NP-40 lysis buffer (50mM Tris-HCl [pH 7.5], 150mM NaCl, 0.5% NP-40). Total cell protein is quantified using the Bradford assay and 1-mg/mL protein aliquots are made. Ten microliters of total cell protein is mixed with 290μL of substrate solution (0.1mg/mL dithiothreitol [DTT], 0.1mg/mL albumin, and 1mM alanine-β- naphthylamide). Fluorometric measurements (340 nm excitation, 400 nm emission) are made after 15 and 30 min. The slope of the line between the 15- and 30-min measurements is used to represent aminopeptidase activity. Total cell protein is preincubated with bestatin, amastatin, puromycin, EDTA, and/or ZnCl2 for 20 min before the fluorometric aminopeptidase assay |
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Cell Assay |
Growing cells (1×106 to 2×106 cells/mL) are diluted to 1.0×103 cells/mL and transferred (3 mL) into a well in a 12-well multiwell plate (2.5-cm diameter/well). Cells are treated with 0, 10, 50, 100, 300, or 600μM Bestatin and allowed to grow at 21°C shaking at 180 rpm for 48 h. A hemocytometer is used to measure cell density after 0, 24, and 48 h. |
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Animal Administration |
Bestatin is dissolved in PBS. The agent (doses of 10, 1, and 0.1mg/kg) is injected i.p. to non-cyclophosphamide-treated mice, 5 or 10 times at 24-h intervals before SRBC immunization. The mice are immunized 24 h after the last dose of bestatin. Pharmacological immunosuppression is induced by a single intraperitoneal injection of cyclophosphamide administered at a dose of 350mg/kg, 12 days before SRBC immunization. Bestatin at the doses of 1 and 0.1mg/kg is injected to cyclophosphamide-immunosuppressed mice i.p. five times at 48-h intervals or 10 times at 24-h intervals before SRBC immunization. The first dose of bestatin is administered 24 h after cyclophosphamide, while the last dose of the drug is injected 24h before SRBC immunization |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
