| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
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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].
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|---|---|
| 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].
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| References |
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| Additional Infomation |
Diaveridine is an aminopyrimidine in which the pyrimidine ring carries amino substituents at C-2 and C-4 and a 3,4-dimethoxybenzyl group at C-5. A folic acid antagonist, it is used as a synergist with sulfonamides against the parasitic Eimeria species. It has a role as an antiparasitic agent and a drug allergen.
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| 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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