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Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $77 | In Stock | |
10 mg | $127 | In Stock | |
25 mg | $263 | In Stock | |
50 mg | $517 | In Stock | |
1 mL x 10 mM (in DMSO) | $85 | In Stock |
Description | L-655708 is a selective and highly potent GABAA receptor reverse agonist with a Ki value of 0.45 nM. |
Targets&IC50 | GABAA:0.45 nM (Ki) |
In vitro | L655708, a potent and selective inverse agonist, targets the benzodiazepine site of GABAA receptors that contain the α5 subunit (Ki = 0.45 nM). It exhibits remarkable selectivity, with a 50-100-fold preference for GABAA receptors containing α1, α2, α3, or α6 subunits when combined with β3 and γ2. In a mouse hippocampal slice model, L655708 enhances long-term potentiation (LTP) and improves spatial learning. Notably, it does so without displaying proconvulsant activity. |
In vivo | At an intraperitoneal administration of 0.7 mg/kg, L-655708 achieves 60-70% occupancy of α5 GABAA receptors, with minimal binding to GABAA receptors containing α1, α2, and α3 subunits. Furthermore, there are no significant off-target behavioral effects, such as sedation and motor impairment. |
Molecular Weight | 341.36 |
Formula | C18H19N3O4 |
Cas No. | 130477-52-0 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 5 mg/mL (14.65 mM), Sonication is recommended. H2O: Insoluble | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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