[CAS NO. 56776-32-0] Etifoxinehydrochloride

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PRODUCTS SPECIFICATIONS [56776-32-0]

Catalog

HY-16579

Brand

MCE

CAS

56776-32-0

DESCRIPTION [56776-32-0]

Overview

MDL	-
Molecular Weight	337.24
Molecular Formula	C17H18Cl2N2O
SMILES	ClC1=CC=C2C(C(C3=CC=CC=C3)(C)OC(NCC)=N2)=C1.Cl

For research use only. We do not sell to patients.

1 Publications Citing Use of MCE

[1]Front Mol Neurosci. 24 May 2022

Summary

Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABA _A receptors . Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents ^[1] ^[2] ^[3] .

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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Etifoxine competitively inhibits [ ³⁵ S]TBPS binding with micromolar potency in rat brain ^[1] .
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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Six-week old BALB/cByJ and C57BL/6J mice (20-25 g) ^[3] .
Dosage:	3.125-50 mg/kg.
Administration:	Intraperitoneal inhection.
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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT03850301	Imperial College London	Multiple Sclerosis	April 1, 2018	Not Applicable
NCT02147548	Biocodex	Healthy Volunteers	December 2013	Phase 3

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 148.26 mM ; Need ultrasonic)

H ₂ O : 5 mg/mL ( 14.83 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

4H-3,1-Benzoxazin-2-amine, 6-chloro-N-ethyl-4-methyl-4-phenyl-, hydrochloride (1:1)

4H-3,1-Benzoxazin-2-amine, 6-chloro-N-ethyl-4-methyl-4-phenyl-, monohydrochloride

Etifoxine hydrochloride

Stresam