Bestatin|58970-76-6|(乌苯美司; Ubenimex)-陌孚医药/Medlife

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Bestatin (Synonyms: 乌苯美司; Ubenimex)

目录号: PC65655 纯度: ≥99%

CAS No. :58970-76-6

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中文名称	Bestatin
中文别名	乌苯美司;N-[(2S,3R)-3-氨基-2-羟基-4-苯丁酰]-L-亮氨酸;贝他定;贝他定(苯丁抑制素);乌苯美司(乌苯美司);乌苯美司-D5(乌苯美司-D5);乌苯美司-D7(乌苯美司-D7);乌苯美司对照品;乌苯美司及其中间体;抑氨肽酶;抑氨肽酶,乌苯美司,贝他定;([2S,3R]-3-氨基-2-羟基-4-苯基丁酰基)-L-亮氨酸;[S-(R,S)]-N-(3-氨基-2-羟基-1-氧代-4-苯丁基)-L-亮氨酸;N -[（2S,3R）-3 -氨基- 2-羟基- 4-苯基丁酰] -L 亮氨酸;N-[(2S,3R)-3-氨基-2-羟基-4-苯基丁酰基]-L-亮氨酸;乌苯美司,N-[(2S,3R)-3-氨基-2-羟基-4-苯基丁酰基]-L-亮氨酸
英文名称	Bestatin
英文别名	ubenimex;(S)-2-((2S,3R)-3-Amino-2-hydroxy-4-phenylbutanamido)-4-methylpentanoic acid;[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutyryl]-L-leucine;[(2S003R)-3-Amino-2-hydroxy-4-phenylbutyryl]-L-leucine;BESTATIN;N-((2S,3R)-3-AMINO-2-HYDROXY-4-PHENYLBUTYRYL)-L-LEUCINE;N-[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutyryl]-L-leucine;BENIMEX;Bestatin,UbeniMex;nk421;[S-(R,S)]-N-(3-Amino-2-hydroxy-1-oxo-4-phenylbuty1)-L-leucine;Direnavir;Bestatin;Ubenimex;Ubenimexum [Latin];Ubenimex (Bestatin);Ubenimex [INN:JAN];Ubenimex(Bestatin);NK 421;I0J33N5627;3-(R)-Amino-2-(S)-hydroxy-4-phenylbutanoyl-(S)-leucine;[(2s,3r)-3-amino-2-hydroxy-4-phenylbutanoyl]-l-leucine;N-[(2S,3R)-3-Amino-2-hydroxy-4
Cas No.	58970-76-6
分子式	C₁₆H₂₄N₂O₄
分子量	308.37
包装储存	4°C, sealed storage and away from moisture；*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage and away from moisture)；

生物活性	Bestatin is a natural, broad-spectrum, and competitive CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase inhibitor. Bestatin has anticancer effects.
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% and 39.93% of control

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

运输条件

Room temperature or refrigerated transport.

储存方式

4°C, sealed storage and away from moisture；*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage and away from moisture)；

ClinicalTrial

结构分类

Ketones, Aldehydes, Acids

来源

Streptomyces olivoreticuli

溶解度数据	体外研究: DMSO : 8.33 mg/mL(27.01 mM;Need ultrasonic) 配制储存液

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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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