5-Fluoroorotic acid
Based on 1 Customer Validation
5-Fluoroorotic acid is the inhibitor for thymidylate synthase that acts as a selective agent in yeast molecular genetics. 5-Fluoroorotic acid exhibits antimalarial activity.
For research use only. We do not sell to patients.
- Purity: 99.17%
- CAS No.: 703-95-7
- Formula: C5H3FN2O4
- Molecular Weight:174.09
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All Parasite Isoforms
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Biological Activity
5-Fluoroorotic acid (1 mg/mL, 4-7 days) inhibits thymidylate synthase, selectively inhibits the growth of Ura+ cells with the presence of UMP synthase, and can be used for screening of Ura- mutated yeast (such as Saccharomyces cerevisiae)[1][3].
5-Fluoroorotic acid (1 nM-100 μM, 48 h) exhibits antimalarial activity against Plasmodium falciparum with an IC50 of 6.0 nM. 5-Fluoroorotic acid exhibits relatively lower cytotoxicity in mammalian cell HT-1080 with an IC50 of 10 μM[4][5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-1080
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Concentration:1 nM-100 μM
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Incubation Time:48 h
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Result:Inhibited cell proliferation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:P. yoelii-infected mouse models[5]
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Dosage:0.2-5 mg/kg
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Administration:ip, every 4 hours for 3 days
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Result:Eliminated malarial parasites.
Caused weight loss, diarrhea, decreased numbers of leukocytes, and increased mortality (5 mg/kg).
Chemical Information
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CAS No. 703-95-7
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Appearance Solid
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Molecular Weight 174.09
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Formula C5H3FN2O4
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Color Off-white to light brown
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SMILES
O=C(C(NC1=O)=C(F)C(N1)=O)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (574.42 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.08 mg/mL (11.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (11.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Boeke JD, et, al. 5-Fluoroorotic acid as a selective agent in yeast molecular genetics. Methods Enzymol. 1987; 154: 164-75. [Content Brief]
[2]. Nikolova K, et, al. Studies on the antimycotic activity of 5-fluoroorotic acid. Methods Find Exp Clin Pharmacol. 1987 Feb; 9(2): 85-9. [Content Brief]
[3]. Santoso D, et al., Fluoroorotic acid-selected Nicotiana plumbaginifolia cell lines with a stable thymine starvation phenotype have lost the thymine-regulated transcriptional program. Plant Physiol. 2000 Aug;123(4):1517-24. [Content Brief]
[4]. Rathod PK, et al., Selective activity of 5-fluoroorotic acid against Plasmodium falciparum in vitro. Antimicrob Agents Chemother. 1989 Jul;33(7):1090-4. [Content Brief]
[5]. Gómez ZM, et al., Antimalarial activity of a combination of 5-fluoroorotate and uridine in mice. Antimicrob Agents Chemother. 1990 Jul;34(7):1371-5. [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 | 5.7442 mL | 28.7208 mL | 57.4416 mL | 143.6039 mL |
| 5 mM | 1.1488 mL | 5.7442 mL | 11.4883 mL | 28.7208 mL | |
| 10 mM | 0.5744 mL | 2.8721 mL | 5.7442 mL | 14.3604 mL | |
| 15 mM | 0.3829 mL | 1.9147 mL | 3.8294 mL | 9.5736 mL | |
| 20 mM | 0.2872 mL | 1.4360 mL | 2.8721 mL | 7.1802 mL | |
| 25 mM | 0.2298 mL | 1.1488 mL | 2.2977 mL | 5.7442 mL | |
| 30 mM | 0.1915 mL | 0.9574 mL | 1.9147 mL | 4.7868 mL | |
| 40 mM | 0.1436 mL | 0.7180 mL | 1.4360 mL | 3.5901 mL | |
| 50 mM | 0.1149 mL | 0.5744 mL | 1.1488 mL | 2.8721 mL | |
| 60 mM | 0.0957 mL | 0.4787 mL | 0.9574 mL | 2.3934 mL | |
| 80 mM | 0.0718 mL | 0.3590 mL | 0.7180 mL | 1.7950 mL | |
| 100 mM | 0.0574 mL | 0.2872 mL | 0.5744 mL | 1.4360 mL |