| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
Azauracil targets enzymes involved in nucleoside synthesis. It inhibits enzymes that are involved in purine and pyrimidine biosynthesis. This inhibition depletes the intracellular GTP and UTP pools. By depleting these nucleotide pools, azauracil inhibits the growth of various microorganisms.
|
|---|---|
| ln Vitro |
In vitro, azauracil inhibits the growth of various microorganisms by depleting intracellular GTP and UTP nucleotide pools. It is used as a growth inhibitor of various microorganisms. Its ability to inhibit nucleotide biosynthesis makes it a useful tool for studying transcriptional elongation and other cellular processes.
|
| ln Vivo |
In vivo, azauracil causes alterations in nucleotide pool levels. It has been widely used in investigations on modulation of transcription, especially in yeast models. It is being used to identify mutations in transcriptional elongation machinery, as well as mutations in a variety of other pathways.
|
| Enzyme Assay |
The activity of azauracil can be assessed using cell-free enzyme assays. The enzymes involved in purine and pyrimidine biosynthesis are incubated with their substrates and cofactors in the presence of varying concentrations of azauracil. The production of nucleotides is measured using chromatographic or spectrophotometric methods. The IC50 for enzyme inhibition is determined from dose-response curves.
|
| Cell Assay |
To evaluate the cellular effects of azauracil, microorganisms or cultured cells are treated with the compound, and the levels of GTP and UTP are measured using HPLC or LC-MS. Cell growth and viability are assessed using standard assays. The effects on transcription can be measured using reporter gene assays or by analyzing RNA levels.
|
| Animal Protocol |
In vivo studies with azauracil typically involve administration to yeast or other model organisms. The compound's effects on growth, nucleotide levels, and transcription are assessed. In yeast, azauracil is used to identify mutations in genes involved in transcriptional elongation.
|
| ADME/Pharmacokinetics |
Azauracil has a molecular formula of C3H3N3O2 and a molecular weight of 113.07. Its CAS number is 461-89-2. The compound is a pyrimidine analog of uracil. It is soluble in water and organic solvents. The purity is typically ≥98%.
|
| Toxicity/Toxicokinetics |
Specific toxicology data for azauracil are not detailed in the available literature. However, as a nucleotide synthesis inhibitor, it can be toxic to rapidly dividing cells. It is considered a research tool and is not used as a therapeutic agent.
|
| Additional Infomation |
6-azauracil is a 1,2,4-triazine compound with oxygen substituents at positions 3 and 5. It is an antimetabolite, belonging to the 1,2,4-triazine class of compounds, and is also a nucleobase analog.
Azauracil (6-AU) is a pyrimidine analog of uracil that exhibits antitumor activity. It is an inhibitor of enzymes involved in purine and pyrimidine biosynthesis. It is widely used in research to study transcriptional elongation and nucleotide metabolism. It is not a clinically approved drug. |
| Molecular Formula |
C3H3N3O2
|
|---|---|
| Molecular Weight |
113.07482
|
| Exact Mass |
113.022
|
| CAS # |
461-89-2
|
| PubChem CID |
68037
|
| Appearance |
White to off-white solid powder
|
| Density |
1.9±0.1 g/cm3
|
| Boiling Point |
503.4ºC at 760 mmHg
|
| Melting Point |
274-275 °C(lit.)
|
| Flash Point |
258.3ºC
|
| Index of Refraction |
1.749
|
| LogP |
-0.59
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
8
|
| Complexity |
162
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
SSPYSWLZOPCOLO-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C3H3N3O2/c7-2-1-4-6-3(8)5-2/h1H,(H2,5,6,7,8)
|
| Chemical Name |
2H-1,2,4-triazine-3,5-dione
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~884.41 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 8.8441 mL | 44.2204 mL | 88.4408 mL | |
| 5 mM | 1.7688 mL | 8.8441 mL | 17.6882 mL | |
| 10 mM | 0.8844 mL | 4.4220 mL | 8.8441 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.