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ADX 10059 hydrochloride
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。
ADX 10059 hydrochloride图片
CAS NO:757949-98-7
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
Negative allosteric modulator at mGlu5
Cas No.757949-98-7
化学名2-((3-fluorophenyl)ethynyl)-4,6-dimethylpyridin-3-amine hydrochloride
Canonical SMILESCC1=CC(C)=NC(C#CC2=CC(F)=CC=C2)=C1N.Cl
分子式C15H13FN2.HCl
分子量276.74
溶解度<6.92mg/ml in Water;<27.67mg/ml in DMSO
储存条件Desiccate at RT
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

ADX 10059 hydrochloride is a potent and selective negative allosteric modulator of mGlu5 receptor with IC50 value of 17.1 nM [1].

Metabotropic glutamate receptor 5 (mGlu5 receptor) is a G protein-coupled receptor and is a receptor for glutamate, which is a primary neurotransmitter involved in signaling in the central nervous system [2].

ADX 10059 hydrochloride is a potent and selective mGlu5 receptor negative allosteric modulator. In patients with migraine, ADX10059 caused pain-free response in 16.1% patients compared with placebo of 4.5% [1]. In patients with gastro-oesophageal reflux disease (GORD) underwent 24-h oesophageal pH-metry, ADX10059 (250 mg) significantly reduced the percentage of acid exposure time with pH< 4 from 7.2% to 3.6%. Also, ADX 10059 significantly decreased the duration and number of symptomatic reflux episodes and reduced oesophageal acid exposure [2].

References:
[1].  Marin JC, Goadsby PJ. Glutamatergic fine tuning with ADX-10059: a novel therapeutic approach for migraine Expert Opin Investig Drugs, 2010, 19(4): 555-561.
[2].  Keywood C, Wakefield M, Tack J. A proof-of-concept study evaluating the effect of ADX10059, a metabotropic glutamate receptor-5 negative allosteric modulator, on acid exposure and symptoms in gastro-oesophageal reflux disease. Gut, 2009, 58(9): 1192-1199.