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AZD-8529 mesylate
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。
AZD-8529 mesylate图片
CAS NO:1314217-69-0
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
AZD-8529 mesylate 是一种有效的,高度选择性的,可口服的 mGluR2 正向调节剂,EC50 值为 285 nM;在 20-25 M 的浓度范围内,对 mGluR1,3,4,5,6,7 和 8 没有正向调节作用。
Cas No.1314217-69-0
Canonical SMILESO=C1C2=C(C)C=C(C3=NC(CN4CCNCC4)=NO3)C=C2CN1CC5=CC=C(OC(F)(F)F)C=C5.OS(=O)(C)=O
分子式C25H28F3N5O6S
分子量583.58
溶解度DMSO: 41.67 mg/mL (71.40 mM)
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

AZD-8529 mesylate is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes[1].

AZD-8529 mesylate potentiates the effects of glutamate at mGluR2 with an EC50 of 195 nM [1].AZD-8529 mesylate does not elicit antagonist responses on mGluRs at 25 μM[1].

AZD-8529 mesylate (0.3-mg/kg, i.m.) reduces nicotine priming-induced and cue-induced reinstatement in squirrel monkeys[1]. AZD-8529 mesylate (30 mg/kg; i.p.) decreases the increased extracellular dopamine induced by nicotine in accumbens shell of freely-moving rats[1]. Animal Model: Sprague-Dawley rats[1]

[1]. Justinova Z, et al. The Novel Metabotropic Glutamate Receptor 2 Positive Allosteric Modulator, AZD8529, Decreases Nicotine Self-Administration and Relapse in Squirrel Monkeys. Biol Psychiatry. 2015 Oct 1;78(7):452-62.