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Bestatin trifluoroacetate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Bestatin trifluoroacetate图片
CAS NO:223763-80-2
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品名称
乌苯美司三氟乙酸盐
Ubenimex trifluoroacetate
产品介绍
Bestatin trifluoroacetate (Ubenimex trifluoroacetate) 是CD13 (Aminopeptidase N)/APNleukotriene A4 hydrolase抑制剂,常用于癌症研究。
生物活性

Bestatin trifluoroacetate is an inhibitor ofCD13 (Aminopeptidase N)/APNandleukotriene A4 hydrolase, used forcancerresearch.

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
分子量

422.40

Formula

C18H25F3N2O6

CAS 号

223763-80-2

中文名称

乌苯美司三氟乙酸盐

结构分类
  • Ketones, Aldehydes, Acids
来源

Streptomyces olivoreticuli

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.