產(chǎn)品目錄

規(guī)格	5mg 10mg 50mg
CAS	951650-22-9
別名
化學(xué)名	3'-(5-(2-hydroxypropan-2-yl)-1H-benzo[d]imidazol-1-yl)-[1,1'-biphenyl]-2-carbonitrile
分子式	C23H19N3O
分子量	353.42
溶解度	≥ 35.3mg/mL in DMSO with gentle warming
儲(chǔ)存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

NS 11394 is a selective GABA(A) receptor-positive modulator.

Preclinical studies suggest that GABAA-1, 2, and 5-containing receptors can mediate the sedative/ motor-impairing, anxiolytic, and memory impairing effects, respectively.

In vitro: Previous study showed that NS11394 possessed a functional selectivity profile at GABA(A) receptors of alpha(5) > alpha(3) > alpha(2) > alpha(1) based on oocyte electrophysiology with human GABA(A) receptors. Moreover, compared with other subtype-selective ligands, NS11394 was unique in having superior efficacy for GABA(A)-alpha(3) receptors while maintaining low efficacy for GABA(A)-alpha(1) receptors [1].

In vivo: Animal study showed that NS11394 had an excellent PK profile, which correlated with pharmacodynamic endpoints of CNS receptor occupancy. In addition, it was showd that NS11394 was potent and highly effective in rodent anxiety models. The anxiolytic efficacy of NS11394 was most probably mediated via its high efficacy at GABA(A)-alpha(3) receptors, though the contribution of GABA(A)-alpha(2) receptors could not be excluded. Moreover, when compared with benzodiazepines, NS11394 had a significantly reduced side effect profile in rat and mouse, even at full CNS receptor occupancy. The authors attributed such benign side effect profile to very low efficacy of NS11394 at GABA(A)-alpha(1) receptors and a partial agonist profile of receptor subtypes. It was also found that NS11394 could impair memory in both rats and mice, which was possibly attributable to its efficacy at GABA(A)-alpha(5) receptors [1].

Clinical trial: Up to now, NS 11394 is still in the preclinical development stage.

特別提醒：

1. 本產(chǎn)品僅供科研使用。請(qǐng)勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請(qǐng)勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請(qǐng)穿好實(shí)驗(yàn)服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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