Size | Price | Stock | Qty |
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5g |
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10g |
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25g |
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50g |
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Other Sizes |
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Uridine triacetate (PN-401; RG 2133; Vistogard; Vistonuridine; Xuriden; Triacetyluridine; TAU), a prodrug of uridine, is an approved medication used for treatment of hereditary orotic aciduria or to treat patients following an overdose of chemotherapy drugs 5-fluorouracil or capecitabine. The acetyl groups of Vistonuridine increase the lipophilicity of uridine, thus enhancing its transport from the gastrointestinal tract to the blood stream and its reabsorption from the renal tubules, while rendering Vistonuridine resistant to catabolism by UrdPase. Uridine triacetate was granted breakthrough therapy designation by FDA in 2015. Uridine triacetate is a prodrug of uridine.
ln Vitro |
In HeLa cells overexpressing ENT1 and ENT2, uridine triacetate inhibits [3H]uridine absorption with IC50 values of 228.4 μM and 28.4 μM, respectively [4].
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ln Vivo |
The oral administration of uridine triacetate (2 g/kg) once every 8 hours for a total of 15 doses has been shown to enhance survival and decrease toxicity in 5-FU overdose mice [3]. Oral administration of uridine triacetate (2 g/kg) once every 8 hours for a total of 15 doses has been shown to decrease 5-FU toxicity and increase the survival rate of DPD-deficient mice [3].
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Animal Protocol |
Animal/Disease Models: 5-FU overdose (intraperitoneal, 300 mg/kg) BALB/c mouse model [3]
Doses: 2 g/kg Route of Administration: po (oral gavage), once every 8 hrs (hrs (hours)), a total of 15 total doses. Experimental Results: The survival rates of the groups initiated within 24, 48, 72, 96, 120 and 144 hrs (hrs (hours)) increased to 90%, 60%, 30%, 20%, 0% and 0% respectively. Animal/Disease Models: 5-ethynyluracil-induced (intraperitoneal (ip) injection, 2 mg/kg) DPD (dihydropyrimidine dehydrogenase)-deficient mouse model [3] Doses: 2 g/kg Route of Administration: po (oral gavage), every 8 hrs (hrs (hours)) Once, 15 times in total. Experimental Results: Starting 4 hrs (hrs (hours)) after 5-FU, the survival rate increased to 100%, and starting within 24 hrs (hrs (hours)), the survival rate increased to 80%. Survival rates improved to 40%, 50%, 20%, 30% and 0% in groups initiated within 48, 72, 96, 120 and 144 hrs (hrs (hours)), respectively. |
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.
[2]. Cada DJ, et al. Uridine Triacetate. Hosp Pharm. 2016 Jun;51(6):484-8. [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. [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. |
Molecular Formula |
C15H18N2O9
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Molecular Weight |
370.3114
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CAS # |
4105-38-8
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SMILES |
O1[C@]([H])(C([H])([C@]([H])([C@@]1([H])C([H])([H])OC(C([H])([H])[H])=O)OC(C([H])([H])[H])=O)OC(C([H])([H])[H])=O)N1C([H])=C([H])C(N([H])C1=O)=O
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~270.04 mM)
H2O : ~10 mg/mL (~27.00 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.75 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.75 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 24 mg/mL (64.81 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.7004 mL | 13.5022 mL | 27.0044 mL | |
5 mM | 0.5401 mL | 2.7004 mL | 5.4009 mL | |
10 mM | 0.2700 mL | 1.3502 mL | 2.7004 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.