EF-5
目录号 : GC33348
EF-5(EF5;2-Nitroimidazole)是用于鉴定细胞缺氧的缺氧标记试剂。
Cas No.:152721-37-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Rats: The rat is given EF-5 as an intravenous injection of 10 mM EF-5 prepared in 0.9% saline. The mass of solution administered is 1% of the rat's mass. Three hours following EF-5 administration, anaesthesia is induced with xylazine and ketamine, the tumor removed and immediately cooled. The tumor is weighed and then bisected. Half of the tumor is used for disaggregation and cell analysis and the other half is quickly frozen for histopathological analysis[2]. |
References: [1]. Wang J, et al. The 2-nitroimidazole EF5 is a biomarker for oxidoreductases that activate the bioreductive prodrug CEN-209 under hypoxia. Clin Cancer Res. 2012 Mar 15;18(6):1684-95. | |
EF-5 (EF5; 2-Nitroimidazole) is a hypoxia labeling agent used to identify hypoxia in cells.
Overexpression of CYPOR induces similar 2- to 4-fold increases in EF-5 binding and metabolic reduction of tirapazamine and CEN-209 in SiHa and HCT116 cell lines, and similar enhancement of γH2AX formation. EF-5 binding and metabolic reduction of the prodrugs are highly correlated in a panel of 14 hypoxic tumor cell lines[1].
EF-5 binding is a promising stratification biomarker for benzotriazine-N-oxide bioreductive prodrugs. In HCT116 xenografts, CYPOR overexpression also significantly increases EF-5 binding and CEN-209 reduction, and modification of tumor hypoxia causes similar changes to the bioreductive activation of both agents, resulting in a strong correlation between EF-5 binding and CEN209-induced DNA damage at the individual tumor level[1]. Following intravenous injection of EF-5, binding and detection using a monoclonal antibody in 9L gliomas is specific and oxygen dependent. Detection of binding using fluorescence microscopy can be performed on frozen tissues; tissue sections can be counterstained with haematoxylin and eosin for light microscopic analysis. Alternatively, the distribution of hypoxia in a tumor can be inferred by examining individual tumor cells using flow cytometric techniques[2].
[1]. Wang J, et al. The 2-nitroimidazole EF5 is a biomarker for oxidoreductases that activate the bioreductive prodrug CEN-209 under hypoxia. Clin Cancer Res. 2012 Mar 15;18(6):1684-95. [2]. Evans SM, et al. Identification of hypoxia in cells and tissues of epigastric 9L rat glioma using EF5 [2-(2-nitro-1H-imidazol-1-yl)-N-(2,2,3,3,3-pentafluoropropyl) acetamide]. Br J Cancer. 1995 Oct;72(4):875-82.
| Cas No. | 152721-37-4 | SDF | |
| Canonical SMILES | O=C(NCC(F)(F)C(F)(F)F)CN1C=CN=C1[N+]([O-])=O | ||
| 分子式 | C8H7F5N4O3 | 分子量 | 302.16 |
| 溶解度 | DMSO : 125 mg/mL (413.69 mM) | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3095 mL | 16.5475 mL | 33.095 mL |
| 5 mM | 0.6619 mL | 3.3095 mL | 6.619 mL |
| 10 mM | 0.331 mL | 1.6548 mL | 3.3095 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Pneumonia cases following an EF-5 tornado
Am J Infect Control 2015 Jul 1;43(7):682-5.PMID:25868649DOI:10.1016/j.ajic.2015.02.027.
Background: Infections following a natural disaster such as an EF-5 tornado can be atypical and difficult to treat. Studies have looked at illness following several natural disasters, but few have studied respiratory illness following a tornado. Materials and methods: A review of patients with pneumonia admitted during the period from May 22, 2009, through May 21, 2012, was completed. The Tornado Zone Group included adult patients who lived or worked in the tornado zone during the year following the tornado. Data were isolated by number of pneumonia cases within and outside the tornado zone per month per year. Results: An analysis of variance comparing the number of pneumonia cases from the tornado zone per month per year was significant at F2,38 = 12.93 and P < .001, with increased cases in the Tornado Zone Group (P < .05). A t test comparing age of pneumonia patients found Tornado Zone patients to be younger than controls (t390 = 5.14; P < .01). Microbes isolated from the Tornado Zone Group included uncommon pathogens not isolated during the 2 years prior. Discussion: The number of pneumonia cases may increase following tornadoes. Although current guidelines recommend narrow-spectrum antibiotics for community-acquired pneumonia, results of this study suggest the possible need for broader antimicrobial coverage after tornadoes.
Hypoxia imaging agents labeled with positron emitters
Recent Results Cancer Res 2013;194:285-99.PMID:22918765DOI:10.1007/978-3-642-27994-2_15.
Imaging hypoxia using positron emission tomography (PET) is of great importance for therapy of cancer. [(18)F]Fluoromisonidazole (FMISO) was the first PET agent for hypoxia imaging, and various radiolabeled nitroimidazole derivatives such as [(18)F]fluoroerythronitroimidazole (FETNIM), [(18)F]1-α-D: -(2-deoxy-2-fluoroarabinofuranosyl)-2-nitroimidazole (FAZA), [(18)F]2-(2-nitro-1H-imidazol-1-yl)-N-(2,2,3,3,3-pentafluoropropyl) acetamide (EF-5), and [(18)F]fluoroetanidazole (FETA) have been developed successively. To overcome the high cost of cyclotron installation, (68)Ga-labeled nitroimidazole derivatives also have been developed. Another important hypoxia imaging agent is (64)Cu-diacetyl-bis(N (4)-methylthiosemicarbazone) ((64)Cu-ATSM), which can distribute in cancer tissue rapidly due to high lipophilicity. However, its application is limited due to high cost of radionuclide production. Although various hypoxia imaging agents have been reported and tested, hypoxia PET images still have to be improved, because of the low blood flow in hypoxic tissues and resulting low uptake of the agents.
Preventing post-disaster population losses and recovery policy
J Emerg Manag 2021 May-Jun;19(3):240-244.PMID:34195977DOI:10.5055/jem.0580.
Objective: On May 22, 2011, an EF-5 tornado struck Joplin, Missouri, leaving behind 161 fatalities and $2.8 billion in economic impacts. This case study of the 2011 disaster was an attempt at determining if and how economic recovery occurred following the disaster through the lived experiences of government officials, local policymakers, and business officials. Design: Case study using in-depth, semistructured, one-on-one interviews and a qualitative design and analysis. Setting: Joplin, Missouri/2011 Joplin Tornado Participants: Seven local government officials, policymakers, and business officials from the city of Joplin that were directly involved in the response and recovery from the 2011 tornado. Interventions: N/A Main outcome measure(s): N/A Results: Policies and actions that were the most effective focused on housing, personal financial resources of the survivors, and ensuring that the recovery processes were expedited as much as prudently possible. Conclusions: Specific policy measures are not recommended through the un-generalizable findings of this case study; however, this case study places a foundation for future research to develop specific policy measures related to disaster recovery.
Novel tyrosinase inhibitory peptide with free radical scavenging ability
J Enzyme Inhib Med Chem 2019 Dec;34(1):1633-1640.PMID:31496313DOI:10.1080/14756366.2019.1661401.
Tyrosinase is a key enzyme involved in melanin synthesis. Therefore, various tyrosinase inhibitors have been screened by researchers in recent years. In the present study, we discovered a novel tyrosinase inhibitor, a peptide ECGYF (named EF-5), with free radical scavenging ability. The effect of tyrosinase inhibition by EF-5 was stronger than that of arbutin and glutathione, when analyzed both in vitro (IC50: 0.46 mM) and in vivo. The UV-Vis absorption and circular dichroism spectroscopies indicated that EF-5 interacted with tyrosinase in a different way as that of glutathione. The results of molecular docking showed that the binding between EF-5 and tyrosinase was determined majorly by hydrogen bonds and hydrophobic interactions. EF-5 had also retained its ability to scavenge both hydroxyl and superoxide radicals in vitro and was found to be nontoxic to cells, as revealed by the MTT assay. These features suggested that the EF-5 peptide may serve as a safe and effective alternative as a tyrosinase inhibitor.
Both ALG-2 and peflin, penta-EF-hand (PEF) proteins, are stabilized by dimerization through their fifth EF-hand regions
Arch Biochem Biophys 2002 Mar 1;399(1):12-8.PMID:11883899DOI:10.1006/abbi.2001.2736.
ALG-2 (apoptosis-linked gene-2 protein) and peflin are Ca(2+)-binding proteins and belong to the penta-EF-hand (PEF) protein family, which includes calpain, sorcin, and grancalcin. ALG-2 forms either a homodimer or a heterodimer with peflin like other PEF proteins. In this study, we found that the fifth-EF-hand (EF-5) regions of both ALG-2 and peflin are essential for dimerization and their stabilities. Exogenously expressed EF-5-deletion (DeltaEF-5) mutants of ALG-2 and peflin were unstable and were not detected in HEK293 cells by Western blotting. In a pulse--chase experiment, the DeltaEF-5 mutants were rapidly degraded, but they were stabilized by treatment with a proteasome inhibitor, MG132. In MG132-treated cells, DeltaEF-5 mutants were recovered in the insoluble fractions. Transient coexpression of ALG-2 increased the peflin level. These results indicate that the absence of a fifth EF-hand results in rapid degradation by the proteasome. On the other hand, stable expression of exogenous peflin decreased the amount of endogenous peflin. The amount of peflin that can dimerize with ALG-2 seems to be restricted in mammalian cells.