计算溶液所需的质量、体积或浓度。
活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
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货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
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B165318-100mg |
100mg |
现货 ![]() |
| |
B165318-500mg |
500mg |
现货 ![]() |
|
别名 | 贝他定 |
---|---|
英文别名 | (3-Amino-2-hydroxy-4-phenylbutanoyl)-L-leucine | UBENIMEX [WHO-DD] | 4-methyl-pyrimidin-2-ylamine | L-Leucine, N-[(2S,3R)-3-amino-2-hydroxy-1-oxo-4-phenylbutyl]- | KBioGR_000273 | N-[(2S,3R)-3-Amino-2-hydroxy-1-oxo-4-phenylbutyl]-L-leucine | SMR000059165 |
规格或纯度 | Moligand™, ≥97% |
英文名称 | Bestatin |
生化机理 | 强大的竞争性氨肽酶抑制剂(亮氨酸氨肽酶和氨肽酶B的IC 50值分别为20和60 nM)。抑制白三烯A 4水解酶和肿瘤细胞增殖。在体内显示免疫调节作用。 |
储存温度 | -20°C储存 |
运输条件 | 超低温冰袋运输 |
作用类型 | 抑制剂 |
作用机制 | 亮氨酸氨肽酶 3 抑制剂;白三烯 A 4 水解酶抑制剂 |
备注 | 如果有可能,您尽量在使用的当天配置溶液,并在当天使用完它。但是,如果您需要预先配制储备溶液,我们建议您将溶液等份保存在-20°C的密封小瓶中。通常,它们最多可以使用一个月。在使用前和打开样品瓶之前,我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度,用法和处理的建议吗?请访问我们的常见问题(FAQ)页面以获取更多详细信息。 |
产品介绍 |
氨基肽酶的抑制剂。急、慢性细胞性白血病等病的辅助 A competitive inhibitor of aminopeptidases, especially aminopeptidase B, leucine aminopeptidase and tripeptide aminopeptidase. Not an inhibitor of carboxypeptidases. |
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作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
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PubChem SID | 504754646 |
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EC号 | 261-529-2 |
分子类型 | 小分子 |
IUPAC Name | (2S)-2-[[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]amino]-4-methylpentanoic acid |
INCHI | InChI=1S/C16H24N2O4/c1-10(2)8-13(16(21)22)18-15(20)14(19)12(17)9-11-6-4-3-5-7-11/h3-7,10,12-14,19H,8-9,17H2,1-2H3,(H,18,20)(H,21,22)/t12-,13+,14+/m1/s1 |
InChi Key | VGGGPCQERPFHOB-RDBSUJKOSA-N |
Canonical SMILES | CC(C)CC(C(=O)O)NC(=O)C(C(CC1=CC=CC=C1)N)O |
Isomeric SMILES | CC(C)C[C@@H](C(=O)O)NC(=O)[C@H]([C@@H](CC1=CC=CC=C1)N)O |
WGK Germany | 3 |
RTECS | OH2915000 |
PubChem CID | 72172 |
分子量 | 308.37 |
溶解性 | Soluble in water (<1 25), DMSO (2 mg/ml), methanol (5 mg/ml), 1eq. NaOH (50 mM), ethanol (<1 mg/ml at 25°C), acetic acid, aq. HCl, and alkaline solution. Insoluble in ethyl acetate, benzene, hexane, and chloroform |
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密度 | 1.197 |
比旋光度 | -19° (C=1,1mol/L HCl) |
熔点 | >200 °C |
分子量 | 308.370 g/mol |
XLogP3 | -1.000 |
氢键供体数Hydrogen Bond Donor Count | 4 |
氢键受体数Hydrogen Bond Acceptor Count | 5 |
可旋转键计数Rotatable Bond Count | 8 |
精确质量Exact Mass | 308.174 Da |
单同位素质量Monoisotopic Mass | 308.174 Da |
拓扑极表面积Topological Polar Surface Area | 113.000 Ų |
重原子数Heavy Atom Count | 22 |
形式电荷Formal Charge | 0 |
复杂度Complexity | 367.000 |
同位素原子数Isotope Atom Count | 0 |
定义的原子立体中心计数Defined Atom Stereocenter Count | 3 |
未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
所有立体化学键的总数The total count of all stereochemical bonds | 0 |
共价键合单元计数Covalently-Bonded Unit Count | 1 |
象形图 | GHS07 |
---|---|
信号词 | Warning |
危险声明 |
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 |
预防措施声明 |
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛:用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出,取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染:用水充分清洗。 P321: 特殊处理(请参阅此标签上的...)。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P271: 仅在室外或通风良好的地方使用。 P304+P340: 如误吸入:将人转移到空气新鲜处,保持呼吸舒适体位。 P403+P233: 存放在通风良好的地方。保持容器密闭。 P362+P364: 脱掉沾污的衣服,清洗后方可重新使用。 P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。 P337+P317: 如果眼睛刺激持续:寻求医疗帮助。 P332+P317: 如果出现皮肤刺激:请寻求医疗帮助。 P319: 如果你感到不适,请寻求医疗帮助。 |
WGK Germany | 3 |
RTECS | OH2915000 |
Merck Index | 9842 |
个人防护装备 | Eyeshields,Gloves,type N95 (US),type P1 (EN143) respirator filter |
Melting point | >200(℃) |
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Purity(HPLC) | 97-100(%) |
Appearance(B165318) | White to Off-White Solid, Powder, or Crystals |
Specific Rotation [a]20/D(c=1 in 1mol/L NaOH) | -13~-9(°) |
Proton NMR spectrum | Conforms to Structure |
1. Yinghua Liu, Jianfeng Zeng, Qing Li, Minqian Miao, Zhuorun Song, Min Zhao, Qingqing Miao, Mingyuan Gao. (2022) An APN-Activated Chemiluminescent Probe for Image-Guided Surgery of Malignant Tumors. Advanced Optical Materials, 10 (14): (2102709). [10.1002/adom.202102709] |
2. Xiao-lin Hou, Xiang Dai, Jie Yang, Bin Zhang, Dong-hui Zhao, Chao-qing Li, Zhong-yuan Yin, Yuan-di Zhao, Bo Liu. (2020) Injectable polypeptide-engineered hydrogel depot for amplifying the anti-tumor immune effect induced by chemo-photothermal therapy. Journal of Materials Chemistry B, 8 (37): (8623-8633). [PMID:32821893] [10.1039/D0TB01370F] |
1. K Ota. (1991-01-01) Review of ubenimex (Bestatin): clinical research.. Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, 45 ((2-3)): (55-60). [PMID:1912370] |
2. Mohammed Alamgir Sarker,Shinji Matsuda,Osamu Mizutani,Shengbin Rao,Koshiro Migita,Nami Goto-Yamamoto,Haruyuki Iefuji,Toshihide Nishimura. (2011-06-15) Purification and characterization of porcine skeletal muscle aminopeptidase T, a novel metallopeptidase homologous to leukotriene A4 hydrolase.. Bioscience, biotechnology, and biochemistry, 75 ((6)): (1154-1159). [PMID:21670530] |
3. Kunio Fujiwara,Masashi Shin,Yohei Yoshizaki,Tsubasa Miyazaki,Tetsuya Saita. (2011-10-19) Immunocytochemistry for bestatin and its application to drug accumulation studies in rat intestine and kidney.. Journal of molecular histology, 42 ((6)): (589-596). [PMID:22006287] |
4. Xi-Jun Qian,Mao-Fang Lin. (2011-11-02) [Effect of APN/CD13 on bestatin enhancing all-trans-retinoic acid-inducing differentiation in NB4 cells].. Zhongguo shi yan xue ye xue za zhi, 19 ((5)): (1125-1128). [PMID:22040956] |
5. Jung-Mi Kang,Hye-Lim Ju,Jung-Won Ju,Woon-Mok Sohn,Tong-Soo Kim,Young-Yil Bahk,Sung-Jong Hong,Byoung-Kuk Na. (2011-12-14) Comparative biochemical and functional properties of two leucine aminopeptidases of Clonorchis sinensis.. Molecular and biochemical parasitology, 182 ((1-2)): (17-26). [PMID:22155540] |
6. Daniela P Alves,Patrícia G da Motta,Patrícia P Lima,Celso M Queiroz-Junior,Marcelo V Caliari,Daniela F Pacheco,Cinthia F Pacheco,Janetti N Francischi,Igor D G Duarte. (2012-01-13) Inflammation mobilizes local resources to control hyperalgesia: the role of endogenous opioid peptides.. Pharmacology, 89 ((1-2)): (22-28). [PMID:22236644] |
7. Magdalena Lis,Bożena Obmińska-Mrukowicz. (2012-02-24) Effects of bestatin on phagocytic cells in cyclophosphamide-treated mice.. Pharmacological reports : PR, 63 ((6)): (1481-1490). [PMID:22358096] |
8. Arun Kumar Singh,Rochika Singh,Dhanendra Tomar,Chirayu D Pandya,Rajesh Singh. (2012-03-14) The leucine aminopeptidase of Staphylococcus aureus is secreted and contributes to biofilm formation.. International journal of infectious diseases : IJID : official publication of the International Society for Infectious Diseases, 16 ((5)): (e375-e381). [PMID:22410279] |
9. Ines Martin-Padura,Paola Marighetti,Alice Agliano,Federico Colombo,Leyre Larzabal,Miriam Redrado,Anne-Marie Bleau,Celia Prior,Francesco Bertolini,Alfonso Calvo. (2012-05-02) Residual dormant cancer stem-cell foci are responsible for tumor relapse after antiangiogenic metronomic therapy in hepatocellular carcinoma xenografts.. Laboratory investigation; a journal of technical methods and pathology, 92 ((7)): (952-966). [PMID:22546866] |
10. Atsushi Wakita,Shigeki Ohtake,Satoru Takada,Fumiharu Yagasaki,Hirokazu Komatsu,Yasushi Miyazaki,Kohmei Kubo,Yukihiko Kimura,Akihiro Takeshita,Yoko Adachi,Hitoshi Kiyoi,Takuhiro Yamaguchi,Minoru Yoshida,Kazunori Ohnishi,Shuichi Miyawaki,Tomoki Naoe,Ryuzo Ueda,Ryuzo Ohno. (2012-05-29) Randomized comparison of fixed-schedule versus response-oriented individualized induction therapy and use of ubenimex during and after consolidation therapy for elderly patients with acute myeloid leukemia: the JALSG GML200 Study.. International journal of hematology, 96 ((1)): (84-93). [PMID:22639053] |
11. Alan H M Wong,Dongxia Zhou,James M Rini. (2012-08-31) The X-ray crystal structure of human aminopeptidase N reveals a novel dimer and the basis for peptide processing.. The Journal of biological chemistry, 287 ((44)): (36804-36813). [PMID:22932899] |
12. Magdalena Lis,Marianna Szczypka,Agnieszka Suszko,Bożena Obmińska-Mrukowicz. (2012-09-11) The effects of bestatin on humoral response to sheep erythrocytes in non-treated and cyclophosphamide-immunocompromised mice.. Immunopharmacology and immunotoxicology, 35 ((1)): (133-138). [PMID:22957713] |
13. Zeng Wang,Jin Xiang,Qin Yu,Mao-Zhi Liang,Feng Nan,Yong-Ping Qin. (2012-09-25) [Determination of ubenimex in human plasma by HPLC-MS/MS].. Sichuan da xue xue bao. Yi xue ban = Journal of Sichuan University. Medical science edition, 43 ((4)): (609-611). [PMID:22997907] |
14. Sebastian D Parlee,Jenna O McNeil,Shanmugam Muruganandan,Christopher J Sinal,Kerry B Goralski. (2012-12-12) Elastase and tryptase govern TNFα-mediated production of active chemerin by adipocytes.. PloS one, 7 ((12)): (e51072-e51072). [PMID:23227233] |
15. Jian-Wei Xu,Cheng-Guang Li,Xin-En Huang,Ying Li,Jie-Ge Huo. (2011-07-28) Ubenimex capsule improves general performance and chemotherapy related toxicity in advanced gastric cancer cases.. Asian Pacific journal of cancer prevention : APJCP, 12 ((4)): (985-987). [PMID:21790238] |
16. Michael B Harbut,Geetha Velmourougane,Seema Dalal,Gilana Reiss,James C Whisstock,Ozlem Onder,Dustin Brisson,Sheena McGowan,Michael Klemba,Doron C Greenbaum. (2011-08-17) Bestatin-based chemical biology strategy reveals distinct roles for malaria M1- and M17-family aminopeptidases.. Proceedings of the National Academy of Sciences of the United States of America, 108 ((34)): (E526-E534). [PMID:21844374] |
17. Florian Veillard,Ahlame Saidi,Roberta E Burden,Christopher J Scott,Ludovic Gillet,Fabien Lecaille,Gilles Lalmanach. (2011-09-08) Cysteine cathepsins S and L modulate anti-angiogenic activities of human endostatin.. The Journal of biological chemistry, 286 ((43)): (37158-37167). [PMID:21896479] |
18. M Lis,M Szczypka,A Suszko,B Obmińska-Mrukowicz. (2011-10-01) Influence of bestatin, an inhibitor of aminopeptidases, on T and B lymphocyte subsets in mice.. Polish journal of veterinary sciences, 14 ((3)): (393-403). [PMID:21957733] |
19. Yanna Zhu,Qiang Meng,Changyuan Wang,Qi Liu,Huijun Sun,Taiichi Kaku,Kexin Liu. (2012-01-26) Organic anion transporters involved in the excretion of bestatin in the kidney.. Peptides, 33 ((2)): (265-271). [PMID:22273603] |
20. Ching-Feng Huang,Chia-Hsiang Chu,Chia-Chao Wu,Zo-Nan Chang,Fung-Lin Chue,Ho-Jen Peng. (2012-01-31) Induction of specific Th1 responses and suppression of IgE antibody formation by vaccination with plasmid DNA encoding Cyn d 1.. International archives of allergy and immunology, 158 ((2)): (142-150). [PMID:22286313] |
21. Xiaopan Zhang,Lei Zhang,Jian Zhang,Jinhong Feng,Yumei Yuan,Hao Fang,Wenfang Xu. (2012-03-03) Design, synthesis and preliminary activity evaluation of novel 3-amino-2-hydroxyl-3-phenylpropanoic acid derivatives as aminopeptidase N/CD13 inhibitors.. Journal of enzyme inhibition and medicinal chemistry, 28 ((3)): (545-551). [PMID:22380779] |
22. Anja Schreiter,Carmen Gore,Dominika Labuz,Marie-Claude Fournie-Zaluski,Bernard P Roques,Christoph Stein,Halina Machelska. (2012-08-28) Pain inhibition by blocking leukocytic and neuronal opioid peptidases in peripheral inflamed tissue.. FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 26 ((12)): (5161-5171). [PMID:22923332] |
23. ChuanYun Dai,Ya Fu,ShaoCheng Chen,Biao Li,Bo Yao,WanHong Liu,LiQing Zhu,Nan Chen,Ji Chen,Qiang Zhang. (2013-01-15) Preparation and evaluation of a new releasable PEGylated tumor necrosis factor-α (TNF-α) conjugate for therapeutic application.. Science China. Life sciences, 56 ((1)): (51-58). [PMID:23314867] |
24. Florian Veillard,Barbara Potempa,Marcin Poreba,Marcin Drag,Jan Potempa. (2013-05-15) Gingipain aminopeptidase activities in Porphyromonas gingivalis.. Biological chemistry, 393 ((12)): (1471-1476). [PMID:23667904] |
25. Yinghua Liu, Jianfeng Zeng, Qing Li, Minqian Miao, Zhuorun Song, Min Zhao, Qingqing Miao, Mingyuan Gao. (2022) An APN-Activated Chemiluminescent Probe for Image-Guided Surgery of Malignant Tumors. Advanced Optical Materials, 10 (14): (2102709). [10.1002/adom.202102709] |
26. Xiao-lin Hou, Xiang Dai, Jie Yang, Bin Zhang, Dong-hui Zhao, Chao-qing Li, Zhong-yuan Yin, Yuan-di Zhao, Bo Liu. (2020) Injectable polypeptide-engineered hydrogel depot for amplifying the anti-tumor immune effect induced by chemo-photothermal therapy. Journal of Materials Chemistry B, 8 (37): (8623-8633). [PMID:32821893] [10.1039/D0TB01370F] |