| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Etifoxine has a dual mechanism of action. First, it potentiates GABA-A receptor-mediated responses. This is mediated by a direct allosteric effect on the receptor's beta subunit and is flumazenil-insensitive, distinguishing it from benzodiazepines. Second, it activates peripheral (mitochondrial-type) benzodiazepine receptors, which enhances neurosteroid synthesis.
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| ln Vitro |
Etefosine (EFX) increases [3H]muscimol binding at equilibrium in a dose-dependent manner at concentrations between 10 and 300 μM (higher concentrations limit its solubility); at 300 μM, EFX 21 reaches 155± of its control value.
In vitro, etifoxine potentiates GABA-A receptor function in cultured neurons. It modulates GABAergic synaptic transmission and increases GABAergic neurotransmission. Its effects are mediated by both a direct allosteric effect on the receptor and an indirect mechanism involving neurosteroid synthesis. |
| ln Vivo |
At micromolar concentrations, etifoxine competitively inhibits [35S]TBPS binding in rat brain [1]. When compared to C57BL/6J mice, BALB/cByJ mice show more pronounced anxiolytic and anticonvulsant effects when exposed to etifoxine (3.125-50 mg/kg) [3].
In vivo, etifoxine has demonstrated anxiolytic properties in anticonflict tests in rats. Its anxiolytic effect is mediated by the neurosteroid allopregnanolone. Etifoxine also possesses neuroprotective and anti-inflammatory properties in vivo. It is used clinically for the treatment of anxiety. |
| Enzyme Assay |
Non-cellular receptor binding assays for etifoxine involve competitive radioligand binding displacement studies using membrane preparations from brain tissue or cells expressing GABA-A receptors. Membranes are incubated with a radiolabeled GABA-A receptor ligand (e.g., [³H]flunitrazepam) and varying concentrations of etifoxine. Binding displacement curves are generated to determine its affinity for the allosteric site.
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| Cell Assay |
In vitro cellular assays for etifoxine involve treating cultured rat neurons with the compound and measuring GABA-A receptor-mediated membrane responses using patch-clamp electrophysiology. Neurons are treated with submaximal concentrations of GABA in the presence of varying concentrations of etifoxine, and the potentiation of the GABA-induced current is measured. The EC₅₀ for potentiation is determined.
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| Animal Protocol |
Animal/Disease Models: Sixweeks old BALB/cByJ and C57BL/6J mice (20-25 g) [3].
Doses: 3.125-50 mg/kg. Route of Administration: intraperitonealinfection. Experimental Results: The 12.5 mg/kg dose of BALB/cByJ mice Dramatically increased arm open time compared to vehicle (p = 0.009), but had no effect in C57B/6J mice. BALB/cByJ mice demonstrated Dramatically (p < 0.012) lower plasma compound levels at 15 and 30 min compared with C57BL/6J mice. In vivo animal experiments with etifoxine are conducted in rat models of anxiety, such as the anticonflict test. Rats are treated with etifoxine via oral or intraperitoneal administration, and their behavior in conflict paradigms is assessed. The compound's effects on neurosteroid levels in the brain are measured. Its neuroprotective effects are assessed in models of neurodegeneration. |
| ADME/Pharmacokinetics |
Etifoxine hydrochloride has a molecular weight of 323.22 and a molecular formula of C₁₇H₁₈Cl₂N₂O. It is a solid powder with a purity of ≥98%. The compound is soluble in DMSO and is typically stored at -20°C, protected from light and moisture. It is orally bioavailable.
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| Toxicity/Toxicokinetics |
Etifoxine is generally well-tolerated at therapeutic doses. Side effects are mild and may include drowsiness, dizziness, and gastrointestinal disturbances. It is contraindicated in patients with known hypersensitivity to the drug. Standard safety precautions should be followed when handling the compound.
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| References |
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| Additional Infomation |
Etifoxine hydrochloride (HOE-36801; CAS 56776-32-0) is a non-benzodiazepine anxiolytic with a dual mechanism of action: positive allosteric modulation of GABA-A receptors and activation of neurosteroid synthesis via peripheral benzodiazepine receptors. It is used clinically for anxiety and has neuroprotective and anti-inflammatory properties.
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| Molecular Formula |
C17H18CL2N2O
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|---|---|
| Molecular Weight |
337.24362
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| Exact Mass |
336.079
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| CAS # |
56776-32-0
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| Related CAS # |
Etifoxine;21715-46-8
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| PubChem CID |
135413552
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| Appearance |
White to off-white solid powder
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| Density |
1.2g/cm3
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| Boiling Point |
421.2ºC at 760mmHg
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| Flash Point |
208.5ºC
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| LogP |
4.859
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
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| Complexity |
394
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SCBJXEBIMVRTJE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H17ClN2O.ClH/c1-3-19-16-20-15-10-9-13(18)11-14(15)17(2,21-16)12-7-5-4-6-8-12/h4-11H,3H2,1-2H3,(H,19,20)1H
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| Chemical Name |
6-chloro-N-ethyl-4-methyl-4-phenyl-4H-benzo[d][1,3]oxazin-2-amine hydrochloride
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| Synonyms |
HOE 36801 HOE-36801 HOE36801 etafenoxine Stresam
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~50 mg/mL (~148.26 mM)
H2O : ~5 mg/mL (~14.83 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.41 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 (7.41 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 (7.41 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 | 2.9652 mL | 14.8262 mL | 29.6525 mL | |
| 5 mM | 0.5930 mL | 2.9652 mL | 5.9305 mL | |
| 10 mM | 0.2965 mL | 1.4826 mL | 2.9652 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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