贝他定 促销 ≥98%(HPLC)
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| 包装规格: | 10mg 100mg 1g in glass bottle |
| 溶解性: | 溶于DMSO(10mg/mL) 。 |
| 产品描述: | 基本信息 产品编号: B10062 产品名称: Bestatin CAS: 58970-76-6 储存条件 粉末 -20℃ 四年 分子式: C16H24N2O4 溶于液体 -80℃ 两年 分子量 308.38 -20℃ 一个月 化学名: (S)-2-((2S,3R)-3-amino-2-hydroxy-4-phenylbutanamido)-4-methylpentanoic acid Solubility (25°C): 体外: DMSO 4mg/mL(12.97mM) Ethanol Insoluble Water Insoluble 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:≥0.83mg/mL(2.69mM);Clear solution 此⽅案可获得≥0.83mg/mL(2.69mM,饱和度未知)的澄清溶液。以1mL⼯作液为例,取100μL8.3mg/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。 2.请依序添加每种溶剂:10% DMSO→90% (20% SBE-β-CD in saline) Solubility:≥0.83mg/mL(2.69mM);Clear solution 此⽅案可获得≥0.83mg/mL(2.69mM,饱和度未知)的澄清溶液。以1mL⼯作液为例,取100μL8.3mg/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 3.请依序添加每种溶剂:10% DMSO→90% corn oil Solubility:≥0.83mg/mL(2.69mM);Clear solution 此⽅案可获得≥0.83mg/mL(2.69mM,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100μL8.3mg/mL的澄清DMSO储备液加到900μL⽟⽶油中,混合均匀。 <1mg/ml表示微溶或不溶。 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。 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。 制备储备液 浓度 溶液体积 质量 1mg 5mg 10mg 1mM 3.2429mL 16.2143mL 32.4286mL 5mM 0.6486mL 3.2429mL 6.4857mL 10mM 0.3243mL 1.6214mL 3.2429mL 生物活性 产品描述 一种CD13(氨肽酶)抑制剂。 靶点 Aminopeptidase-N 体外研究 Bestatin抑制除KG1的所有的人白血病细胞系的增殖。在U937细胞中,Bestatin诱导DNA片段化和DNA梯及增强caspase-3的活性。Bestati剂量依赖性诱导人白血病细胞系中的DNA片段化。Bestatin剂量依赖性抑制SN12M细胞侵袭进入重组基底膜(基质胶)。Bestatin浓度依赖性抑制肿瘤细胞的IV型胶原的退化,但不通过肿瘤条件培养基(TCM)。在SN12M细胞中,Bestatin抑制朝着氨肽酶的底物水解活性。Bestatin抑制人脐静脉内皮细胞(HUVECs)中的管状形成。Bestatin通过固定在细胞表面的亮氨酸氨肽酶对淋巴细胞(和单核细胞)发挥直接的刺激作用,通过氨基肽酶B抑制吞噬作用激素的分解代谢发挥单核细胞(淋巴细胞)的间接作用。 体内研究 Bestatin显著抑制小鼠背部气囊测定黑色素瘤细胞诱导的血管生成。在种植了B16-BL6黑色素瘤细胞的小鼠的背部侧中,Bestatin减少既定原发性肿瘤块血管的数量。在EGDA大鼠的食管组织中,Bestatin统计学显著抑制白三烯B4的生物合成,在EGDA大鼠中,Bestatin降低EAC的发病率,从57.7%至26.1%。 推荐实验方法(仅供参考) 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 290 μL of substrate solution (0.1mg/mL dithiothreitol [DTT], 0.1mg/mL albumin, and 1mM alanine-β- naphthylamide). Fluorometric measurements (340nm excitation, 400nm 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. Cell Assay Growing cells (1×106 to 2×106 cells/mL) are diluted to 1.0×103 cells/mL and transferred (3mL) 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. 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. |
| 保存条件: | -20℃ |
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