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L-655,708

Catalog No.GC17350

inverse agonist for the benzodiazepine site of GABAA receptors containing the α5 subunit

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L-655,708 Chemical Structure

Cas No.: 130477-52-0

Size Price Stock Qty
10mM (in 1mL DMSO)
$87.00
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5mg
$79.00
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10mg
$140.00
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50mg
$558.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

L-655708 is a potent α5 subunit-selective GABAA receptor inverse agonist (Ki = 0.45 nM).IC50: 0.45 nM (Ki)Target: GABAin vitro: L-655708 is a potent, selective inverse agonist for the benzodiazepine site of GABAA receptors containing the α5 subunit (Ki = 0.45 nM). Displays 50-100-fold selectivity over GABAA receptors containing α1, α2, α3 orα6 subunits in combination with β3 and γ2. Enhances LTP in a mouse hippocampal slice model and increases spatial learning, without displaying proconvulsant activity.in vivo: L-655708 at 0.7 mg/kg, administered intraperitoneally, would result in 60-70% occupancy of α5 GABAA receptors with limited binding to α1, α2, and α3 subunit-containing GABAA receptors and no significant off-target behavioral effects, such as sedation and motor impairment.[1]

References:
[1]. Saab BJ, et al. Short-term memory impairment after isoflurane in mice is prevented by the α5 γ-aminobutyric acid type A receptorinverse agonist L-655708. Anesthesiology. 2010 Nov;113(5):1061-1071.

Chemical Properties

Cas No. 130477-52-0 SDF
Chemical Name (S)-ethyl 7-methoxy-9-oxo-11,12,13,13a-tetrahydro-9H-benzo[e]imidazo[5,1-c]pyrrolo[1,2-a][1,4]diazepine-1-carboxylate
Canonical SMILES CCOC(C(N=CN12)=C2[C@]3([H])CCCN3C(C4=C1C=CC(OC)=C4)=O)=O
Formula C18H19N3O4 M.Wt 341.37
Solubility DMF: 2mg/mL,DMF:PBS (pH 7.2) (1:20): 0.04mg/mL,DMSO: 1mg/mL Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.9294 mL 14.6469 mL 29.2937 mL
5 mM 0.5859 mL 2.9294 mL 5.8587 mL
10 mM 0.2929 mL 1.4647 mL 2.9294 mL
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