Etifoxine
Based on 3 publication(s) in Google Scholar
Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents.
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- Pureté : 99.27%
- CAS No.: 21715-46-8
- Formule: C17H17ClN2O
- Masse moléculaire:300.78
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Etifoxine
More
Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Caco-2 | CC50 |
43.53 μM
Compound: ETIFOXINE
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Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
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10.21203/rs.3.rs-23951/v1 |
| Caco-2 | IC50 |
20.64 μM
Compound: ETIFOXINE
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Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
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10.21203/rs.3.rs-23951/v1 |
In Vitro
Etifoxine (EFX), at concentrations ranging from 10 to 300 μM (higher concentrations limited its solubility), produces a dose-dependent increase in the [3H]muscimol binding at equilibrium, to 155±2% of its control value at 300 μM EFX[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Etifoxine (3.125-50 mg/kg) exhibits more pronounced anxiolytic and anticonvulsant effects in the BALB/cByJ mice compared to the C57BL/6J mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six-week old BALB/cByJ and C57BL/6J mice (20-25 g)[3].
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Dosage:3.125-50 mg/kg.
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Administration:Intraperitoneal injection.
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Result:Significantly increased the amount of time spent on the open arms at the 12.5 mg/kg dose when compared to vehicle (p = 0.009) in BALB/cByJ mice but produced no effect in C57B/6J mice.
BALB/cByJ mice compared with C57BL/6J mice exhibited significantly (p < 0.012) lower plasma levels of the compound at 15 and 30 min.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 21715-46-8
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Appearance Solid
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Masse moléculaire 300.78
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Formule C17H17ClN2O
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Color Light yellow to yellow
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SMILES
ClC1=CC=C2C(C(C3=CC=CC=C3)(C)OC(NCC)=N2)=C1
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Synonyms
HOE 36-801
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Front Mol Neurosci
2022 May 24:15:850904. PMID: 35686060 -
Psychopharmacology (Berl)
TSPO activation ameliorates maternal immune activation induced PV interneuron deficits via BDNF/TrkB signaling. [Abstract]2025 Jun;242(6):1303-1319. PMID: 39621042 -
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (332.47 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (8.31 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 (8.31 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (536 KB)
- English - EN (536 KB)
- Français - FR (536 KB)
- Deutsch - DE (536 KB)
- Norwegian - NO (536 KB)
- Español - ES (536 KB)
- Swedish - SV (536 KB)
- Italian - IT (536 KB)
- Korean - KR (536 KB)
- Portuguese - PT (536 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Marc Verleye, et al. Effects of etifoxine on ligand binding to GABA(A) receptors in rodents. Neurosci Res. 2002 Oct;44(2):167-72. [Content Brief]
[2]. Alain Hamon, et al. The modulatory effects of the anxiolytic etifoxine on GABA(A) receptors are mediated by the beta subunit. Neuropharmacology. 2003 Sep;45(3):293-303. [Content Brief]
[3]. Marc Verleye, et al. Differential effects of etifoxine on anxiety-like behaviour and convulsions in BALB/cByJ and C57BL/6J mice: any relation to overexpression of central GABAA receptor beta2 subunits? Eur Neuropsychopharmacol. 2011 Jun;21(6):457-70. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3247 mL | 16.6234 mL | 33.2469 mL | 83.1172 mL |
| 5 mM | 0.6649 mL | 3.3247 mL | 6.6494 mL | 16.6234 mL | |
| 10 mM | 0.3325 mL | 1.6623 mL | 3.3247 mL | 8.3117 mL | |
| 15 mM | 0.2216 mL | 1.1082 mL | 2.2165 mL | 5.5411 mL | |
| 20 mM | 0.1662 mL | 0.8312 mL | 1.6623 mL | 4.1559 mL | |
| 25 mM | 0.1330 mL | 0.6649 mL | 1.3299 mL | 3.3247 mL | |
| 30 mM | 0.1108 mL | 0.5541 mL | 1.1082 mL | 2.7706 mL | |
| 40 mM | 0.0831 mL | 0.4156 mL | 0.8312 mL | 2.0779 mL | |
| 50 mM | 0.0665 mL | 0.3325 mL | 0.6649 mL | 1.6623 mL | |
| 60 mM | 0.0554 mL | 0.2771 mL | 0.5541 mL | 1.3853 mL | |
| 80 mM | 0.0416 mL | 0.2078 mL | 0.4156 mL | 1.0390 mL | |
| 100 mM | 0.0332 mL | 0.1662 mL | 0.3325 mL | 0.8312 mL |
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