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L-655708
🥰Excellent
Catalog No. TQ0151Cas No. 130477-52-0
L-655708 is a selective and highly potent GABAA receptor reverse agonist with a Ki value of 0.45 nM.
L-655708
🥰Excellent
Purity: 98.41%
Catalog No. TQ0151Cas No. 130477-52-0
L-655708 is a selective and highly potent GABAA receptor reverse agonist with a Ki value of 0.45 nM.
| 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 |
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Purity:98.41%
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Product Introduction
Bioactivity
Chemical Properties
| 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 |
| Smiles | [H][C@@]12CCCN1C(=O)c1cc(OC)ccc1-n1cnc(C(=O)OCC)c21 |
| Relative Density. | 1.42 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 5 mg/mL (14.65 mM), Sonication is recommended. H2O: Insoluble | ||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.93 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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