| Size | Price | |
|---|---|---|
| 1mg | ||
| 5mg | ||
| 10mg | ||
| Other Sizes |
| ln Vitro |
Propylene glycol, ethanol, ether, and chloroform are all soluble in dioxone. You can get an aqueous solution with a pH of 4.3 that is 1% at room temperature. One can make a 2% aqueous solution by raising the temperature to 50°C [1].
|
|---|---|
| ln Vivo |
Dioxins (0-30 mg/kg; IV, IP, PO, SC; once) may have a convulsive impact [1].
|
| Animal Protocol |
Animal/Disease Models: CF-1 mice and CF-Wistar rats [1]
Doses: 0-30 mg/kg Route of Administration: One intraperitoneal (ip) injection Experimental Results: Mice: Locomotor activity often diminished, always at 10 mg/kg Tremors, clonic convulsions, and motor incoordination occurred after administration of 30 mg/kg accompanied by high responsiveness. In rats: Tremors and some isolated myoclonus of the limbs were observed at 10 mg/kg, and clonic spasms were seen at doses above 15 mg/kg. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
In rat and rabbit serum, dioxins are mainly bound to globulins, with a small amount bound to albumin. |
| Toxicity/Toxicokinetics |
Interactions
The effects of administering antiepileptic drugs 1–4 days prior to dioxin administration on dioxin-induced seizures were investigated in mice. Administration of methylphenidate, primidone, and metoline 2 days prior to dioxin administration enhanced its effects. Phenytoin sodium exhibited anticonvulsant activity in the first two days; after 4 days, the required dioxin dose to induce seizures in 50 animals decreased. The hypnotic response in 50 mice was used as the titration endpoint, and diethylamine dione was used to titrate the hypnotic drugs pentobarbital sodium and hydroxydione. The antagonistic effect of diethylamine dione on hypnosis may be competitive or non-competitive. This study investigated the dose of amobarbital sodium required to maintain the hypnotic state at the titration endpoint in 50 mice under escalating doses of antistimulants such as bemiglitol, diethylamine dione, picric acid, pentylenetetrazole, and β-spirocyclopentaneglutamate. Except for bitter substances, the titration curves showed a slope reversal at the highest dose, and Diethadione enhanced the inhibitory effect of the hypnotic drugs. These sedatives and hypnotics may both act on the same excitatory synapses, with the former acting as agonists and the latter as competitive or non-competitive antagonists. |
| References |
[1]. G MAFFII, et al. A new analeptic: 5, 5-diethyl-1, 3-oxazine-2,4-dione (Dioxone). J Pharm Pharmacol. 1961 Apr;13:244-53.
|
| Additional Infomation |
Diethadione is an oxazine alkane.
|
| Molecular Formula |
C8H13NO3
|
|---|---|
| Molecular Weight |
171.19
|
| Exact Mass |
171.09
|
| CAS # |
702-54-5
|
| PubChem CID |
12798
|
| Appearance |
CRYSTALS FROM ETHER
|
| Density |
1.069g/cm3
|
| Melting Point |
97-98 °C
|
| Index of Refraction |
1.44
|
| LogP |
1.388
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
12
|
| Complexity |
208
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(N1)OCC(CC)(CC)C1=O
|
| InChi Key |
ORTYMGHCFWKXHO-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C8H13NO3/c1-3-8(4-2)5-12-7(11)9-6(8)10/h3-5H2,1-2H3,(H,9,10,11)
|
| Chemical Name |
5,5-diethyl-1,3-oxazinane-2,4-dione
|
| Synonyms |
HSDB 5514; Diethadionum; Diethadione
|
| 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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~584.15 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (14.60 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 (14.60 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 (14.60 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 | 5.8415 mL | 29.2073 mL | 58.4146 mL | |
| 5 mM | 1.1683 mL | 5.8415 mL | 11.6829 mL | |
| 10 mM | 0.5841 mL | 2.9207 mL | 5.8415 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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