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Lorediplon
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。
Lorediplon图片
CAS NO:917393-39-6
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
Lorediplon 是一种新型的非苯二氮卓类药物,作为 GABAA 受体调节剂,在 α1 亚基上具有差异活性,与促进睡眠有关。
Cas No.917393-39-6
化学名N-[2-fluoro-5-[3-(2-thienylcarbonyl)pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]-N-methyl-acetamide
Canonical SMILESO=C(C1=CC=CS1)C2=C3N(N=C2)C(C4=CC=C(F)C(N(C)C(C)=O)=C4)=CC=N3
分子式C20H15FN4O2S
分子量394.4
溶解度DMF: 25 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 14 mg/ml
储存条件Store at -20°C
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

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]

References:
[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