Fialuridine
Based on 1 Customer Validation
Fialuridine (FIAU), a nucleoside analog, is a HSV-1 and HSV-2 inhibitor with Kis of 0.14 μM and 0.95 μM, respectively. Fialuridine shows anti-orthopoxvirus and anti-hepatitis B virus (HBV) activities. Fialuridine inhibits duck HBV DNA replication with IC50 values of 0.075 μM and 156 μM in human hepatoma cells and in chicken liver cells, respectively.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.98%
- CAS 番号: 69123-98-4
- 分子式: C9H10FIN2O5
- 分子量:372.09
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NC-37 | CC50 |
6.7 μg/mL
Compound: 4
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Cytotoxic concentration required to inhibit NC-37 cells by 50%
Cytotoxic concentration required to inhibit NC-37 cells by 50%
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10.1016/S0960-894X(01)80146-3 |
| NC-37 | EC50 |
0.06 μg/mL
Compound: 4
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Concentration required to reduce HSV-1 (KOS strain) induced cytopathogenicity in NC-37 cells
Concentration required to reduce HSV-1 (KOS strain) induced cytopathogenicity in NC-37 cells
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10.1016/S0960-894X(01)80146-3 |
| RG2 | CC50 |
80 μM
Compound: FIAU
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Cytotoxicity against RG2 cells after 72 hrs by MTT assay
Cytotoxicity against RG2 cells after 72 hrs by MTT assay
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[PMID: 18800764] |
| Sf21 | IC50 |
>1000 μM
Compound: Fialuridine
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Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
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[PMID: 21965623] |
| Sf21 | IC50 |
>1000 μM
Compound: Fialuridine
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Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
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[PMID: 21965623] |
Fialuridine against Vaccinia and Cowpox viruses in HFF cells with EC50 values of 1.5 and 0.2 μM, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 69123-98-4
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性状 Solid
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分子量 372.09
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分子式 C9H10FIN2O5
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Color White to off-white
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SMILES
O[C@H]1[C@H](F)[C@H](N2C(NC(C(I)=C2)=O)=O)O[C@@H]1CO
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別名
FIAU; フィアルウリジン; DRG-0098; NSC 678514
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (268.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.72 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.72 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (276 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Mansuri MM, et al. 1-(2-Deoxy-2-fluoro-beta-D-arabinofuranosyl)-5-ethyluracil. A highly selective antiherpes simplex agent. J Med Chem. 1987 May;30(5):867-71. [Content Brief]
[2]. Mark N Prichard, et al. Orthopoxvirus targets for the development of antiviral therapies. Curr Drug Targets Infect Disord. 2005 Mar;5(1):17-28. [Content Brief]
[3]. Staschke KA, et al. The in vitro anti-hepatitis B virus activity of FIAU [1-(2'-deoxy-2'-fluoro-1-beta-D-arabinofuranosyl-5-iodo)uracil] is selective, reversible, and determined, at least in part, by the host cell. Antiviral Res. 1994 Jan;23(1):45-61. [Content Brief]
[4]. Richardson FC, et al. Fialuridine accumulates in DNA of dogs, monkeys, and rats following long-term oral administration. Proc Natl Acad Sci U S A. 1994 Dec 6;91(25):12003-7. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6875 mL | 13.4376 mL | 26.8752 mL | 67.1880 mL |
| 5 mM | 0.5375 mL | 2.6875 mL | 5.3750 mL | 13.4376 mL | |
| 10 mM | 0.2688 mL | 1.3438 mL | 2.6875 mL | 6.7188 mL | |
| 15 mM | 0.1792 mL | 0.8958 mL | 1.7917 mL | 4.4792 mL | |
| 20 mM | 0.1344 mL | 0.6719 mL | 1.3438 mL | 3.3594 mL | |
| 25 mM | 0.1075 mL | 0.5375 mL | 1.0750 mL | 2.6875 mL | |
| 30 mM | 0.0896 mL | 0.4479 mL | 0.8958 mL | 2.2396 mL | |
| 40 mM | 0.0672 mL | 0.3359 mL | 0.6719 mL | 1.6797 mL | |
| 50 mM | 0.0538 mL | 0.2688 mL | 0.5375 mL | 1.3438 mL | |
| 60 mM | 0.0448 mL | 0.2240 mL | 0.4479 mL | 1.1198 mL | |
| 80 mM | 0.0336 mL | 0.1680 mL | 0.3359 mL | 0.8399 mL | |
| 100 mM | 0.0269 mL | 0.1344 mL | 0.2688 mL | 0.6719 mL |
Fialuridine 関連分類
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