| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
The primary targets of 6-Azathymine include D-3-aminoisobutyrate-pyruvate aminotransferase (EC 2.6.1.40), DNA biosynthesis pathways, and viral polymerases. It is a competitive antagonist of the growth of Streptococcus faecalis and several other strains of microorganisms. It inhibits DNA biosynthesis and has antibacterial and antiviral activities. It is a Mycoplasma genitalium metabolite.
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| ln Vitro |
6-Azathymine inhibits the growth of Streptococcus faecalis (8043) and a number of other microbial strains in a competitive manner. Research on 6-Azathymine's mode of action shows that S. The analog can be changed by faecalis into azathymidine, the equivalent deoxyriboside[2].
In vitro, 6-Azathymine is a competitive antagonist of the growth of Streptococcus faecalis and several other strains of microorganisms. It inhibits DNA biosynthesis and has antibacterial and antiviral activities. The compound is a potent D-3-aminoisobutyrate-pyruvate aminotransferase inhibitor. Its antibacterial and antiviral activities are concentration-dependent and have been demonstrated in standard microbiological assays. |
| ln Vivo |
When the mouse is given 6-Azathymine, both free and different metabolites of the drug are eliminated through the urine. After mice are given 6-Azathymine-5-14C, radioactivity is discovered in every tissue examined. This radioactivity can be identified as metabolic byproducts as well as free Azathymine[3].
In vivo, the administration of 6-Azathymine to mice leads to the urinary elimination not only of free Azathymine, but also of various metabolites of it. The compound inhibits viral polymerase or nucleotide metabolism; resistance develops via substitutions in catalytic or nucleotide-binding residues. Common mutations or resistance-associated sites occur in polymerase active site and nucleotide recognition motifs. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for 6-Azathymine typically involve antimicrobial susceptibility testing. Bacterial strains (e.g., Streptococcus faecalis) are cultured in appropriate media and treated with serial dilutions of the compound. The minimum inhibitory concentration (MIC) is determined after 24-48 hours of incubation at 37°C using the broth microdilution method. The compound demonstrates concentration-dependent antibacterial activity.
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| Cell Assay |
In vitro cellular assays for 6-Azathymine involve testing its antibacterial and antiviral activities. Bacterial cultures and virus-infected cells are treated with serial dilutions of 6-Azathymine (0.1-1000 µg/mL). Cell viability and viral replication are measured by optical density, plaque assay, or qRT-PCR. The minimum inhibitory concentration (MIC) and effective concentration (EC50) are calculated from dose-response curves.
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| Animal Protocol |
In vivo animal studies for 6-Azathymine involve pharmacokinetic and metabolism studies. Mice are administered 6-Azathymine via oral or intraperitoneal routes. Urine is collected and analyzed for free Azathymine and its metabolites using chromatographic methods. The compound leads to the urinary elimination of free Azathymine and various metabolites.
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| ADME/Pharmacokinetics |
6-Azathymine has a molecular formula of C4H5N3O2 and a molecular weight of 127.10. It appears as a solid powder with a purity of ≥95%. It has a melting point of 210-212°C and a density of 1.67±0.1 g/cm3. The compound is soluble in DMSO at 10 mM in vitro. It has a LogP of -0.3, indicating hydrophilicity. It should be stored at room temperature. It is intended for research use only and is not for human consumption.
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| Toxicity/Toxicokinetics |
The toxicity profile of 6-Azathymine has not been extensively characterized. As a nucleobase analogue, it may have cytotoxic effects similar to other antimetabolites. Standard toxicity studies would include assessment of body weight changes, hematological parameters, and histopathological examination of major organs in animal models. The compound is intended for research use only and is not approved for clinical use.
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| References |
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| Additional Infomation |
6-azathymidine is a nucleobase analog, a derivative of thymine in which the CH group at the 6-position is replaced by a nitrogen atom. It is a metabolite of Mycoplasma genitalium and an inhibitor of EC 2.6.1.40 [(R)-3-amino-2-methylpropionic acid-pyruvate transaminase]. It is a cyclic ketone, belonging to the 1,2,4-triazine class of compounds, and is also a nucleobase analog.
6-Azathymine (CAS 932-53-6) is a nucleobase analogue that is thymine in which the CH group at position 6 is replaced by nitrogen. It has a molecular formula of C4H5N3O2 and a molecular weight of 127.10. It is a potent D-3-aminoisobutyrate-pyruvate aminotransferase inhibitor that inhibits DNA biosynthesis and has antibacterial and antiviral activities. It is a competitive antagonist of the growth of Streptococcus faecalis. It is intended for research use only and is not approved for clinical use. |
| Molecular Formula |
C4H5N3O2
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|---|---|
| Molecular Weight |
127.10
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| Exact Mass |
127.038
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| CAS # |
932-53-6
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| PubChem CID |
70269
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| Appearance |
White to off-white solid powder
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| Density |
1.7±0.1 g/cm3
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| Melting Point |
210-212°C
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| Index of Refraction |
1.692
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| LogP |
-2.05
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
9
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| Complexity |
196
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XZWMZFQOHTWGQE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C4H5N3O2/c1-2-3(8)5-4(9)7-6-2/h1H3,(H2,5,7,8,9)
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| Chemical Name |
6-methyl-2H-1,2,4-triazine-3,5-dione
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| HS Tariff Code |
2934.99.9001
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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 : 125 mg/mL (983.48 mM)
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| 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 | 7.8678 mL | 39.3391 mL | 78.6782 mL | |
| 5 mM | 1.5736 mL | 7.8678 mL | 15.7356 mL | |
| 10 mM | 0.7868 mL | 3.9339 mL | 7.8678 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.
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