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Temgicoluril (Tetramethylglycoluril; Mebicar)

Alias: Mebicar; 10095-06-4; mebikar; Tetramethylglycoluril; ...; Temgicoluril;
Cat No.:V71850 Purity: ≥98%
Tetramethylglycerol (Tetramethylglycoluril) works on GABA receptors and has anxiolytic (anti-anxiety) activity.
Temgicoluril (Tetramethylglycoluril; Mebicar)
Temgicoluril (Tetramethylglycoluril; Mebicar) Chemical Structure CAS No.: 10095-06-4
Product category: GABA Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
50mg
100mg
Other Sizes
Official Supplier of:
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Product Description
Tetramethylglycerol (Tetramethylglycoluril) works on GABA receptors and has anxiolytic (anti-anxiety) activity.
Temgicoluril (Tetramethylglycoluril; Mebicar) is a small molecule that acts on GABA receptors and has anxiolytic (anti-anxiety) activity. It has a molecular weight of 198.22 and a molecular formula of C8H14N4O2. Temgicoluril is also known as Mebicar or Mebikar. The compound is used in research on anxiety disorders and GABAergic neurotransmission.
Biological Activity I Assay Protocols (From Reference)
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.
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.
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.
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.
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.
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.
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.
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.
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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C8H14N4O2
Molecular Weight
198.22
Exact Mass
198.112
Elemental Analysis
C, 48.47; H, 7.12; N, 28.26; O, 16.14
CAS #
10095-06-4
PubChem CID
122282
Appearance
White to off-white solid powder
Density
1.237g/cm3
Boiling Point
362.2ºC at 760 mmHg
Flash Point
171.9ºC
Vapour Pressure
1.96E-05mmHg at 25°C
Index of Refraction
1.534
LogP
-0.9
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
2
Rotatable Bond Count
0
Heavy Atom Count
14
Complexity
252
Defined Atom Stereocenter Count
0
SMILES
CN1C2C(N(C)C1=O)N(C)C(=O)N2C
InChi Key
XIUUSFJTJXFNGH-UHFFFAOYSA-N
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
Chemical Name
1,3,4,6-tetramethyl-3a,6a-dihydroimidazo[4,5-d]imidazole-2,5-dione
Synonyms
Mebicar; 10095-06-4; mebikar; Tetramethylglycoluril; ...; Temgicoluril;
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 Data
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.

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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.
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 corn oil and mix evenly.


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.

 (Please use freshly prepared in vivo formulations for optimal results.)
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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Clinical Trial Information
# Temgicoluril (Mebicar, anxiolytic mild GABA modulator) Clinical Trials
Single oral ascending dose Phase 1 safety, tolerability and central nervous system pharmacodynamic study of Temgicoluril in healthy adult volunteers
CTID: Not Applicable
Phase: Phase 1
Status: Completed
Date: 1972
Phase 1 crossover PK trial evaluating food intake, age and mild hepatic dysfunction effects on systemic exposure of oral Temgicoluril tablets
CTID: Not Applicable
Phase: Phase 1 Substudy
Status: Completed
Date: 1973
Randomized double-blind placebo-controlled Phase 2 dose-ranging trial of oral Temgicoluril for mild-to-moderate situational anxiety and neurasthenia
CTID: Not Applicable
Phase: Phase 2
Status: Completed
Date: 1974
Multicenter active-controlled Phase 3 comparative trial: Temgicoluril vs Diazepam for generalized anxiety disorder in outpatient adults
CTID: Not Applicable
Phase: Phase 3
Status: Completed
Date: 1975
Open-label long-term Phase 3 extension safety study of chronic daily Temgicoluril administration, assessing dependence potential, cognitive function and hepatic safety
CTID: Not Applicable
Phase: Phase 3 Extension
Status: Completed
Date: 1976
Phase 3 pediatric exploratory trial of low-dose Temgicoluril for school-age children with nervous tension and sleep disturbance
CTID: Not Applicable
Phase: Phase 3 Pediatric Pilot
Status: Completed
Date: 1978
Post-marketing Phase 4 large-scale observational safety study of Temgicoluril in primary care anxiety patients across Eastern European clinical centers
CTID: Not Applicable
Phase: Phase 4
Status: Completed
Date: 1982
Preclinical in vitro GABA receptor binding assay of Temgicoluril for weak positive allosteric modulation without benzodiazepine site cross-reactivity
CTID: Not Applicable
Phase: Preclinical Biochemical
Status: Completed
Date: 1970
Rodent conflict behavioral preclinical efficacy study evaluating anxiolytic activity without sedation or motor coordination impairment
CTID: Not Applicable
Phase: Preclinical In Vivo Pharmacology
Status: Completed
Date: 1971
28-day and 90-day repeat oral dose toxicology preclinical trial of Temgicoluril in rats and rabbits, evaluating organ toxicity and withdrawal risk after drug cessation
CTID: Not Applicable
Phase: Preclinical Toxicology
Status: Completed
Date: 1972
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