| Size | Price | Stock | Qty |
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| 500mg |
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| Other Sizes |
| Targets |
Diaveridine targets dihydrofolate reductase (DHFR), an enzyme that catalyzes the reduction of dihydrofolate to tetrahydrofolate, a crucial step in the synthesis of nucleotides. By inhibiting DHFR, Diaveridine blocks the production of tetrahydrofolate, which is essential for the synthesis of DNA, RNA, and proteins. This inhibition leads to the disruption of bacterial and protozoal growth, making it effective as an antibacterial and anticoccidial agent.
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| ln Vitro |
Diaveridine is both an antibacterial and a dihydrofolate reductase (DHFR) inhibitor, with a Ki value of 11.5 nM for wild-type DHFR [1]. Salmonella typhimurium TA1535 was strongly bactericidal after being treated with daviridine for 90 minutes; no bacterial growth was seen above 10 μg/mL. Treatment with Diaveridine for 48 hours (but not for 24 hours) significantly increased the frequency of aberrant metaphases in the absence of metabolic activation in a dose-dependent manner. 60% of metaphases have chromosomal abnormalities at 100 μg/mL [2].
In vitro, Diaveridine is a potent inhibitor of DHFR with a Ki of 11.5 nM for the wild-type enzyme. It is used in enzyme assays to study DHFR inhibition and as a reference compound for the development of new DHFR inhibitors. Its antibacterial activity is also assessed in vitro against various bacterial strains. |
| ln Vivo |
The Diaveridine (DVD) treatment group did not exhibit substantially different sperm abnormalities from the negative control group at any of the dose levels (Diaveridine, 128 to 512 mg/kg). The micronuclei of the Diaveridine treatment group (Diaveridine, 128 to 512 mg/kg) and the negative control group did not differ significantly. The chromosomal abnormalities seen in the positive control group treated with cyclophosphamide (P<0.05) and the daviridine treatment group at each dose were considerably smaller than those in the positive control group. This suggests that the daviridine dose under investigation did not result in aberrant chromosome aberrations. At the conclusion of the trial, the findings demonstrated that the administration of diaveridine had no appreciable effect on the organ body weight ratio when compared to the negative control group [3].
In vivo, Diaveridine is used in veterinary medicine as an anticoccidial agent and as an antibacterial synergist. It is often used in combination with other drugs, such as sulfonamides, to enhance their antibacterial activity. Its efficacy in treating coccidiosis in poultry and other animals has been demonstrated. |
| Enzyme Assay |
In vitro enzyme assays for Diaveridine typically measure its ability to inhibit DHFR activity. The enzyme is incubated with its substrate (dihydrofolate) and NADPH in the presence of increasing concentrations of the compound. The reduction of dihydrofolate is measured spectrophotometrically, and IC50 or Ki values are calculated. Diaveridine shows a Ki of 11.5 nM for wild-type DHFR.
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| Cell Assay |
Cell-based assays for Diaveridine involve treating bacterial or protozoal cultures with the compound and measuring its effects on cell growth and viability. Minimum inhibitory concentrations (MICs) are determined to assess its antibacterial and anticoccidial activity. These studies help characterize the compound's spectrum of activity and its potential as a therapeutic agent.
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| Animal Protocol |
In vivo animal studies for Diaveridine are typically conducted in poultry or other animals to evaluate its efficacy in treating coccidiosis and bacterial infections. The compound is administered orally, and its effects on parasite load, bacterial burden, and animal health are assessed. These studies are crucial for determining its clinical efficacy and safety in veterinary medicine.
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| ADME/Pharmacokinetics |
Diaveridine has a molecular weight of 260.29 g/mol and a molecular formula of C13H16N4O2. The compound is stored at -20°C.
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| Toxicity/Toxicokinetics |
The toxicological profile of Diaveridine has been evaluated in veterinary studies. The compound is generally well-tolerated at therapeutic doses. However, as with any drug, appropriate safety precautions should be taken when handling the compound. Its use is limited to veterinary applications.
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| References |
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| Additional Infomation |
Dimethicone is an aminopyrimidine compound with amino substituents at C-2 and C-4 positions and a 3,4-dimethoxybenzyl group at C-5 position of its pyrimidine ring. It is a folic acid antagonist that can synergize with sulfonamides to treat Eimeria coccidiosis. It is both an antiparasitic drug and a drug allergen.
Diaveridine is a veterinary drug with no approved human therapeutic use. It is used as an anticoccidial agent and as an antibacterial synergist in veterinary medicine. Its potent inhibition of DHFR makes it a valuable tool for studying folate metabolism and for developing new antimicrobial agents. |
| Molecular Formula |
C13H16N4O2
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|---|---|
| Molecular Weight |
260.29
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| Exact Mass |
260.127
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| CAS # |
5355-16-8
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| PubChem CID |
21453
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
506.1±60.0 °C at 760 mmHg
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| Melting Point |
232 - 236ºC
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| Flash Point |
259.9±32.9 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.626
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| LogP |
1.09
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
19
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| Complexity |
279
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LDBTVAXGKYIFHO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H16N4O2/c1-18-10-4-3-8(6-11(10)19-2)5-9-7-16-13(15)17-12(9)14/h3-4,6-7H,5H2,1-2H3,(H4,14,15,16,17)
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| Chemical Name |
5-[(3,4-dimethoxyphenyl)methyl]pyrimidine-2,4-diamine
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| Synonyms |
AI3 23935; AI323935; AI3-23935
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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 : ~33.33 mg/mL (~128.05 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.60 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 (9.60 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 (9.60 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8419 mL | 19.2093 mL | 38.4187 mL | |
| 5 mM | 0.7684 mL | 3.8419 mL | 7.6837 mL | |
| 10 mM | 0.3842 mL | 1.9209 mL | 3.8419 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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