Description
L-655708 is a potent α5 subunit-selective GABAA receptor inverse agonist (Ki=0.45 nM).
Product information
CAS Number: 130477-52-0
Molecular Weight: 341.36
Formula: C18H19N3O4
Chemical Name: ethyl (7S)-15-methoxy-12-oxo-2,4,11-triazatetracyclo[11.4.0.0²,⁶.0⁷,¹¹]heptadeca-1(13),3,5,14,16-pentaene-5-carboxylate
Smiles: COC1=CC2=C(C=C1)N1C=NC(=C1[C@@H]1CCCN1C2=O)C(=O)OCC
InChiKey: YKYOQIXTECBVBB-AWEZNQCLSA-N
InChi: InChI=1S/C18H19N3O4/c1-3-25-18(23)15-16-14-5-4-8-20(14)17(22)12-9-11(24-2)6-7-13(12)21(16)10-19-15/h6-7,9-10,14H,3-5,8H2,1-2H3/t14-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 20 mg/mL (58.59 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
L655708 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.
Products are for research use only. Not for human use.
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