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L-655,708
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
L-655,708图片
CAS NO:130477-52-0
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议

产品介绍
L-655,708 是一种有效的 α5 亚基选择性 GABAA 受体反向激动剂 (Ki\u003d0.45 nM)。
Cas No.130477-52-0
化学名(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 SMILESCCOC(C(N=CN12)=C2[C@]3([H])CCCN3C(C4=C1C=CC(OC)=C4)=O)=O
分子式C18H19N3O4
分子量341.37
溶解度DMF: 2mg/mL,DMF:PBS (pH 7.2) (1:20): 0.04mg/mL,DMSO: 1mg/mL
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.