Edoxudine (EUDR)
(Synonyms: 乙去氧尿啶; EUDR) 目录号 : GC32148
Edoxudine (EUDR)是一种脱氧胸苷类似物，已被证实对单纯疱疹病毒1型和2型具有抑制作用。
Cas No.:15176-29-1
Sample solution is provided at 25 µL, 10mM.
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Edoxudine (EUDR) is a deoxy-thymidine analog shown to be effective against herpes simplex virus type 1 and type 2 [1]. Edoxudine has been shown in vertebrate systems to be phosphorylated preferentially by the thymidine kinase and incorporated into viral DNA, and inhibiting viral DNA synthesis[2]. Edoxudine disrupts the outer wall of Klebsiella pneumoniae and damages the protective effect of the LPS layer, making the cell membrane of Klebsiella pneumoniae accessible to antibacterial effectors[3]. Edoxudine has been widely used as a lead compound for the development of drugs targeting the surface protein of monkeypox virus E8 [4].
In vitro, Edoxudine treatment for 72 hours significantly inhibited the proliferation of human foreskin fibroblasts (HFFs), with an IC50 value of 115µM[5].
References:
[1] Sharma A, Tiwari V, Sowdhamini R. Computational search for potential COVID-19 drugs from FDA-approved drugs and small molecules of natural origin identifies several anti-virals and plant products[J]. Journal of biosciences, 2020, 45(1): 100.
[2] Mazzacano C A, Fallon A M. Evaluation of a viral thymidine kinase gene for suicide selection in transfected mosquito cells[J]. Insect molecular biology, 1995, 4(2): 125-134.
[3] Ifrid E, Ouertatani-Sakouhi H, Jauslin T, et al. 5-ethyl-2’-deoxyuridine fragilizes Klebsiella pneumoniae outer wall and facilitates intracellular killing by phagocytic cells[J]. Plos one, 2022, 17(10): e0269093.
[4] Podduturi S, Vemula D, Singothu S, et al. In-silico investigation of E8 surface protein of the monkeypox virus to identify potential therapeutic agents[J]. Journal of Biomolecular Structure and Dynamics, 2024, 42(16): 8242-8255.
[5] Kumar R, Wiebe L I, Knaus E E. Synthesis and antiviral activity of novel 5-(1-azido-2-haloethyl) and 5-(1-azido-, amino-, or methoxyethyl) analogs of 2'-deoxyuridine[J]. Journal of medicinal chemistry, 1993, 36(17): 2470-2474.
Edoxudine (EUDR)是一种脱氧胸苷类似物，已被证实对单纯疱疹病毒1型和2型具有抑制作用[1]。在脊椎动物系统中，Edoxudine可优先被胸苷激酶磷酸化并掺入病毒DNA中，从而抑制病毒DNA的合成[2]。Edoxudine能破坏肺炎克雷伯菌的外壁并损伤其脂多糖层的保护作用，使细菌细胞膜对抗菌效应物更易感[3]。Edoxudine已广泛用作先导化合物，用于开发靶向猴痘病毒E8表面蛋白的药物[4]。
在体外，使用Edoxudine处理人包皮成纤维细胞（HFFs）72小时，显著抑制了细胞增殖，IC50值为115µM [5]。
| Cell experiment [1]: | |
Cell lines | Human foreskin fibroblast (HFF) |
Preparation Method | 24h prior to assay, human foreskin fibroblasts (HFFs) were seeded in 6-well plates at a concentration of 2.5×104 cells per well in MEM containing 10% FBS. The media from the wells was then aspirated with different concentrations of Edoxudine (1, 10, 100, and 1000µM). The cells were incubated in a CO2 incubator at 37°C for 72h. The media-drug solution was removed, and the cells were washed. 1ml of 0.25% trypsin was added to each well and incubated until the cells started to come off of the plate. The cell-media mixture was then pipetted up and down vigorously to break up the cell suspension, followed by cell counting. |
Reaction Conditions | 1, 10, 100, and 1000µM; 72h |
Applications | Edoxudine treatment decreased the cell viability of HFFs in a dose-dependent manner. |
References: | |
| Cas No. | 15176-29-1 | SDF | |
| 别名 | 乙去氧尿啶; EUDR | ||
| Canonical SMILES | OC[C@@H]1[C@H](C[C@H](N2C(NC(C(CC)=C2)=O)=O)O1)O | ||
| 分子式 | C11H16N2O5 | 分子量 | 256.26 |
| 溶解度 | DMSO : ≥ 125 mg/mL (487.79 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 | 3.9023 mL | 19.5114 mL | 39.0229 mL |
| 5 mM | 780.5 μL | 3.9023 mL | 7.8046 mL |
| 10 mM | 390.2 μL | 1.9511 mL | 3.9023 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。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet