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Mavoglurant(AFQ056)
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。
Mavoglurant(AFQ056)图片
CAS NO:543906-09-8
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Mavoglurant (AFQ056) (AFQ056) 是一种有效的、选择性的、非竞争性的、具有口服活性的 mGluR5 拮抗剂,IC50 为 30 nM。
Cas No.543906-09-8
别名(3AR,4S,7AR)-八氢-4-羟基-4-[2-(3-甲基苯基)乙炔基]-1H-吲哚-1-羧酸甲酯,AFQ056
Canonical SMILESCC1=CC(C#C[C@]2(O)CCC[C@]3([H])[C@@]2([H])CCN3C(OC)=O)=CC=C1
分子式C19H23NO3
分子量313.39
溶解度DMSO : ≥ 47 mg/mL (149.97 mM)
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

Mavoglurant is a structurally novel, non-competitive mGlu5 receptor antagonist, has an IC50 of 30 nM in a functional assay with human mGluR5.IC50 value: 30 nMTarget: mGluR5in vitro: Mavoglurant is a selective non-competitive antagonist which showed efficacy in the treatment of L-dopa induced dyskinesias in Parkinson's disease and Fragile X mental retardation in proof of principle studies. Mavoglurant is selective over the other mGluR subtypes, iGluRs and a panel of 238 CNS relevant receptors, transporter or enzymes. [1]In vivo: Mavoglurant shows an improved pharmacokinetic profile in rat and efficacy in the stress-induced hyperthermia test in mice as compared to the prototypic mGluR5 antagonist MPEP.[1]

[1]. Vranesic I, et al. AFQ056/mavoglurant, a novel clinically effective mGluR5 antagonist: identification, SAR and pharmacological characterization. Bioorg Med Chem. 2014 Nov 1;22(21):5790-5803.