L-655708

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

L-655708 是有效的, 选择性 GABAA 受体反向激动剂 (Ki=0.45 nM)。

L-655708 is a potent α5 subunit-selective GABAA receptor inverse agonist (Ki=0.45 nM).

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.

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.

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Others

Other Targets

GABA Receptor

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130477-52-0

341.36

C18H19N3O4

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 10 mg/mL (29.29 mM; 超声助溶 (<60°C)

[H][C@@]12CCCN1C(=O)c1cc(OC)ccc1-n1cnc(C(=O)OCC)c21

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(-20℃)

With Ice Pack

≥ 2 years