Uridine triacetate
Based on 1 Customer Validation
Uridine triacetate (Tri-O-acetyl uridine) is an orally active proagent of Uridine (HY-B1449). Uridine triacetate is quickly absorbed in the gut, and is rapidly deacetylated in the circulation to yield free uridine. Uridine triacetate is used for the research of 5-fluorouracil (5-FU) and capecitabine toxicity, or early-onset cardiac or central nervous system (CNS).
For research use only. We do not sell to patients.
- Purity: 99.88%
- CAS No.: 4105-38-8
- Formula: C15H18N2O9
- Molecular Weight:370.31
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Uridine triacetate inhibits [3H]uridine uptake in ENT1 and ENT2 overexpressed HeLa cells, with IC50s of 28.4 μM and 228.4 μM respectively[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Uridine triacetate (2 g/kg, oral gavage, every 8 h for 15 total doses) improves survival and reduced 5-FU toxicity in DPD deficiency mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:5-FU overdose (i.p., 300 mg/kg) BALB/c mice model[3]
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Dosage:2 g/kg
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Administration:Oral gavage, every 8 h for 15 total doses.
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Result:Improved the survival rate to 90%, 60%,30%, 20%, 0% and 0% in the groups initiated within 24, 48, 72, 96, 120 and 144 h, respectively.
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Animal Model:5-ethynyluracil-induced (i.p., 2mg/kg) DPD (dihydropyrimidine dehydrogenase) deficiency mice model[3]
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Dosage:2 g/kg
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Administration:Oral gavage, every 8 h for 15 total doses.
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Result:Improved the survival rate to 100% when initiated 4 h after 5-FU, 80% when initiated within 24 h.
Improved the survival rate to 40%, 50%,20%, 30% and 0% in groups initiated within 48, 72, 96, 120 and 144 h, respectively.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 4105-38-8
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Appearance Solid
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Molecular Weight 370.31
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Formula C15H18N2O9
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Color White to off-white
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SMILES
O=C1NC(C=CN1[C@H]2[C@H](OC(C)=O)[C@H](OC(C)=O)[C@@H](COC(C)=O)O2)=O
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Synonyms
Tri-O-acetyl uridine
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : ≥ 100 mg/mL (270.04 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 10 mg/mL (27.00 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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: ≥ 2.5 mg/mL (6.75 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 (6.75 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 24 mg/mL (64.81 mM); Clear solution; Need ultrasonic
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 (281 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]. Ma WW, et al. Emergency use of uridine triacetate for the prevention and treatment of life-threatening 5-fluorouracil and capecitabine toxicity. Cancer. 2017 Jan 1;123(2):345-356. [Content Brief]
[2]. Cada DJ, et al. Uridine Triacetate. Hosp Pharm. 2016 Jun;51(6):484-8. [Content Brief]
[3]. Rolando A G Garcia, et al. Prompt treatment with uridine triacetate improves survival and reduces toxicity due to fluorouracil and capecitabine overdose or dihydropyrimidine dehydrogenase deficiency. Toxicol Appl Pharmacol. 2018 Aug 15;353:67-73. [Content Brief]
[4]. Siennah R Miller, et al. Predicting Drug Interactions with Human Equilibrative Nucleoside Transporters 1 and 2 Using Functional Knockout Cell Lines and Bayesian Modeling. Mol Pharmacol. 2021 Feb;99(2):147-162. [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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.7004 mL | 13.5022 mL | 27.0044 mL | 67.5110 mL |
| 5 mM | 0.5401 mL | 2.7004 mL | 5.4009 mL | 13.5022 mL | |
| 10 mM | 0.2700 mL | 1.3502 mL | 2.7004 mL | 6.7511 mL | |
| 15 mM | 0.1800 mL | 0.9001 mL | 1.8003 mL | 4.5007 mL | |
| 20 mM | 0.1350 mL | 0.6751 mL | 1.3502 mL | 3.3756 mL | |
| 25 mM | 0.1080 mL | 0.5401 mL | 1.0802 mL | 2.7004 mL | |
| DMSO | 30 mM | 0.0900 mL | 0.4501 mL | 0.9001 mL | 2.2504 mL |
| 40 mM | 0.0675 mL | 0.3376 mL | 0.6751 mL | 1.6878 mL | |
| 50 mM | 0.0540 mL | 0.2700 mL | 0.5401 mL | 1.3502 mL | |
| 60 mM | 0.0450 mL | 0.2250 mL | 0.4501 mL | 1.1252 mL | |
| 80 mM | 0.0338 mL | 0.1688 mL | 0.3376 mL | 0.8439 mL | |
| 100 mM | 0.0270 mL | 0.1350 mL | 0.2700 mL | 0.6751 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.