Lorediplon

A ligand for α1 subunit-containing GABAA receptors

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库存: 现货

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数量
5mg

￥325.00

260.00

- +
10mg

￥612.00

490.00

- +
25mg

￥1425.00

1140.00

- +
50mg

￥2450.00

1960.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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货号: ajci20840
CAS: 917393-39-6
别名:
分子式: C20H15FN4O2S
分子量: 394.4
纯度: >98%
溶解度: DMF: 25 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 14 mg/ml
储存: Store at -20°C
库存: 现货

Background

Lorediplon is a novel non-benzodiazepine, hypnotic drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.Target: GABALorediplon is a drug for the treatment of insomnia, has been successfully completed with a best-in-class efficacy profile in terms of maintaining sleep and sleep quality, Lorediplon targets GABAA. [1] Lorediplon demonstrates a minimum of 10-fold and 6-fold increase in potency (respectively) in the spontaneous motor activation studies. At concentrations of 1.2mg/kg, Lorediplon demonstrates a 57%increased effect on Slow Wave Sleep (SWS), when compared with a placebo.[2]

参考文献:
[1]. Zisapel N. Current Phase II investigational therapies for insomnia. Expert Opin Investig Drugs. 2015 Mar;24(3):401-411.
[2]. Horoszok L, et al. A single-dose, randomized, double-blind, double dummy, placebo and positive-controlled, five-way cross-over study to assess the pharmacodynamic effects of lorediplon in a phase advance model of insomnia in healthy Caucasian adult male s