| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Temgicoluril targets GABA receptors. By acting on GABA receptors, the compound modulates inhibitory neurotransmission in the central nervous system. Temgicoluril has anxiolytic activity, suggesting that it enhances GABAergic signaling.
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|---|---|
| ln Vitro |
In vitro activity data for Temgicoluril are not extensively documented. The compound acts on GABA receptors and has anxiolytic activity. Further in vitro studies are needed to fully characterize its activity profile and mechanism of action.
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| ln Vivo |
Temgicoluril has been shown to have anxiolytic activity in vivo. It acts on GABA receptors to produce its anti-anxiety effects. Further in vivo studies are needed to fully characterize its efficacy and safety profile.
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| Enzyme Assay |
The in vitro receptor binding assay for Temgicoluril involves measuring its binding to GABA receptors. The assay typically uses radioligand binding techniques. Temgicoluril is incubated with GABA receptors at various concentrations. The IC50 or Ki value is determined by fitting the binding data to a dose-response curve.
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| Cell Assay |
In vitro cellular assays for Temgicoluril typically use cell lines expressing GABA receptors to assess its effects on receptor function. Cells are treated with the compound at various concentrations. Receptor activity is measured using electrophysiological techniques or fluorescent-based assays.
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| Animal Protocol |
In vivo animal experiments for Temgicoluril would typically use animal models of anxiety. The compound would be administered via intraperitoneal or oral routes. Anxiolytic effects would be assessed using behavioral tests such as the elevated plus maze or light/dark test.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Temgicoluril are not extensively documented. As a small molecule with a molecular weight of 198.22, the compound is expected to have reasonable bioavailability. Its imidazole-dione structure may influence its absorption, distribution, metabolism, and excretion. Further pharmacokinetic studies are necessary to fully characterize its PK profile.
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| Toxicity/Toxicokinetics |
Toxicological data for Temgicoluril are not extensively available in the public domain. As a research compound, it has not undergone extensive toxicological evaluation. Standard cytotoxicity assays in cell lines may have been performed to assess safety margins. Further preclinical toxicology studies would be required before clinical development.
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| References |
[1]. Izuchenie osobennosteĭ spektra psikhotropnogo deĭstviia mebikara [Characteristics of the psychotropic spectrum of action of mebicar]. Biull Eksp Biol Med. 1980 May;89(5):568-70. Russian.
[2]. Preventive Effect of Mebicar and Ginsenoside Rg1 on Neurobehavioral and Immunological Disruptions Caused by Intermittent Unpredictable Stress in Mice. Neuroimmunomodulation. 2018;25(1):49-58. |
| Additional Infomation |
Mebicar is an imidazolidinone drug.
Temgicoluril (Tetramethylglycoluril; Mebicar) is a small molecule that acts on GABA receptors and has anxiolytic activity. It has a molecular weight of 198.22. No clinical trials or regulatory approvals have been reported. |
| Molecular Formula |
C8H14N4O2
|
|---|---|
| Molecular Weight |
198.22
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| Exact Mass |
198.112
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| Elemental Analysis |
C, 48.47; H, 7.12; N, 28.26; O, 16.14
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| CAS # |
10095-06-4
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| PubChem CID |
122282
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| Appearance |
White to off-white solid powder
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| Density |
1.237g/cm3
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| Boiling Point |
362.2ºC at 760 mmHg
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| Flash Point |
171.9ºC
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| Vapour Pressure |
1.96E-05mmHg at 25°C
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| Index of Refraction |
1.534
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| LogP |
-0.9
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
14
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| Complexity |
252
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN1C2C(N(C)C1=O)N(C)C(=O)N2C
|
| InChi Key |
XIUUSFJTJXFNGH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H14N4O2/c1-9-5-6(11(3)7(9)13)12(4)8(14)10(5)2/h5-6H,1-4H3
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| Chemical Name |
1,3,4,6-tetramethyl-3a,6a-dihydroimidazo[4,5-d]imidazole-2,5-dione
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| Synonyms |
Mebicar; 10095-06-4; mebikar; Tetramethylglycoluril; ...; Temgicoluril;
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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 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)
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| Solubility (In Vitro) |
DMSO: 125 mg/mL (630.61 mM)
H2O: 100 mg/mL (504.49 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (10.49 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 20.8 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: ≥ 2.08 mg/mL (10.49 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 20.8 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: ≥ 2.08 mg/mL (10.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (504.49 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.0449 mL | 25.2245 mL | 50.4490 mL | |
| 5 mM | 1.0090 mL | 5.0449 mL | 10.0898 mL | |
| 10 mM | 0.5045 mL | 2.5224 mL | 5.0449 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.