Pheneturide
Based on 1 Customer Validation
Pheneturide (Ethylphenacemide; M 551) is an orally active anticonvulsant. Pheneturide is a decarboxylation product of 5-ethyl-5-phenylbarbituric acid, with antiepileptic and central inhibitory effects. Pheneturide has protective effects against both MES tonic convulsions and Metrazol clonic convulsions. Pheneturide prolongs sedative-induced sleep, increases spontaneous locomotor activity, and inhibits fighting behavior. Pheneturide can be used in epilepsy-related research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.20%
- No. CAS: 90-49-3
- Fòrmula: C11H14N2O2
- Peso molecular:206.25
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Actividad biológica
Descripciòn
In Vitro
Pheneturide (1 mM) is inactive against 14C-orotate uptake in Bacillus cereus 569H, with orotate incorporation remaining at 95% of control[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Pheneturide (42.5 mg/kg; oral) inhibits electroshock-induced tonic extensor convulsions in rats[1].
Pheneturide (oral; single dose) inhibits pentylenetetrazol-induced tonic extensor seizures in mice and prevents pentylenetetrazol-induced death[1].
Pheneturide (10% of the oral LD50; oral) prolongs barbiturate-induced sleep time in mice[1].
Pheneturide (150 mg/kg; oral; twice daily; for 3 consecutive days) brings isoproterenol-stimulated pineal NAT activity in rats to 2,428 pmol/pineal/h[3].
Pheneturide (p.o.; single dose; peak effect at 2 hours) antagonizes maximal electroshock-induced convulsive components, with the lowest ED50 for tonic hindlimb extension (45.0 mg/kg)[5].
Pheneturide (p.o.; single dose; peak effect at 2 hours) antagonizes pentylenetetrazol-induced convulsive components, with the lowest ED50 for tonic hindlimb extension (22.2 mg/kg)[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:dd-strain (male, 16-20 g)[1]
-
Dosage:28 mg/kg
-
Administration:oral (p.o.) by stomach tube
-
Result:Oral anti-electroshock ED50 was 28 mg/kg.
NTD50/ED50 ratio was 6.25.
LD50/ED50 ratio was 28.
-
Animal Model:Wistar (male, 150-200 g)[1]
-
Dosage:42.5 mg/kg
-
Administration:oral (p.o.) by stomach tube
-
Result:Oral anti-electroshock ED50 was 42.5 mg/kg.
LD50/ED50 ratio was 28.8.
-
Animal Model:dd-strain (male, 16-20 g)[1]
-
Dosage:10% of oral LD50
-
Administration:oral (p.o.) by stomach tube; 1 and 3 hours before barbiturate 40 mg/kg i.p.
-
Result:Sleep duration was 48 minutes with pheneturide given 1 hour before barbiturate.
Sleep duration was 165 minutes with pheneturide given 3 hours before barbiturate.
-
Animal Model:Wistar (male, 200-250 g)[3]
-
Dosage:150 mg/kg
-
Administration:p.o.; twice daily (0700 and 1645) for 3 days; once 19 h before isoproterenol HCl 12.5 mg/kg
-
Result:In the isoproterenol HCl-stimulated NAT assay, Pheneturide 150 mg/kg p.o. produced NAT activity of 2,428 pmol/pineal/hr.
Chemical Information
-
No. CAS 90-49-3
-
Appearance Solid
-
Peso molecular 206.25
-
Fòrmula C11H14N2O2
-
Color White to off-white
-
SMILES
O=C(NC(N)=O)C(CC)C1=CC=CC=C1
-
Synonyms
Ethylphenacemide; M 551
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (484.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (12.12 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (12.12 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
-
Ficha de datos (289 KB)
-
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.8485 mL | 24.2424 mL | 48.4848 mL | 121.2121 mL |
| 5 mM | 0.9697 mL | 4.8485 mL | 9.6970 mL | 24.2424 mL | |
| 10 mM | 0.4848 mL | 2.4242 mL | 4.8485 mL | 12.1212 mL | |
| 15 mM | 0.3232 mL | 1.6162 mL | 3.2323 mL | 8.0808 mL | |
| 20 mM | 0.2424 mL | 1.2121 mL | 2.4242 mL | 6.0606 mL | |
| 25 mM | 0.1939 mL | 0.9697 mL | 1.9394 mL | 4.8485 mL | |
| 30 mM | 0.1616 mL | 0.8081 mL | 1.6162 mL | 4.0404 mL | |
| 40 mM | 0.1212 mL | 0.6061 mL | 1.2121 mL | 3.0303 mL | |
| 50 mM | 0.0970 mL | 0.4848 mL | 0.9697 mL | 2.4242 mL | |
| 60 mM | 0.0808 mL | 0.4040 mL | 0.8081 mL | 2.0202 mL | |
| 80 mM | 0.0606 mL | 0.3030 mL | 0.6061 mL | 1.5152 mL | |
| 100 mM | 0.0485 mL | 0.2424 mL | 0.4848 mL | 1.2121 mL |