Mavoglurant|543906-09-8|(AFQ056)-陌孚医药/Medlife

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Mavoglurant (Synonyms: AFQ056)

目录号: PL07156 纯度: ≥99%

CAS No. :543906-09-8

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中文名称	Mavoglurant
中文别名	(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;(3Ar,4s,7ar)-甲基 4-羟基-4-(2-间甲苯乙炔)-八氢吲哚-1-羧酸
英文名称	Mavoglurant
英文别名	(3aR,4S,7aR)-Octahydro-4-hydroxy-4-[2-(3-methylphenyl)ethynyl]-1H-indole-1-carboxylic acid methyl ester;Mavoglurant;methyl (3aR,4S,7aR)-4-hydroxy-4-[2-(3-methylphenyl)ethynyl]-3,3a,5,6,7,7a-hexahydro-2H-indole-1-carboxylate;1H-Indole-1-carboxylic acid,octahydro-4-hydroxy-4-(2-(3-methylphenyl)ethynyl)-,methyl ester,(3aR,4S,7aR);AFQ056;AFQ-056;Mavoglurant [INN];UNII-GT0I9SV4F6
Cas No.	543906-09-8
分子式	C₁₉H₂₃NO₃
分子量	313.39
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Mavoglurant (AFQ056) 是一种有效，选择性，非竞争性和口服活性的 mGluR5 拮抗剂，IC₅₀ 值为 30 nM。Mavoglurant 对 mGluR5 显示出 >300 倍的选择性。Mavoglurant 可用于研究脆性 X 综合征 (FXS) 和帕金森氏症中左旋多巴引起的运动障碍。

生物活性

Mavoglurant (AFQ056) is a potent, selective, non-competitive and orally active mGluR5 antagonist, with an IC 50 of 30 nM. Mavoglurant shows a >300 fold selectivity for the mGluR5 over all targets (238) tested. Mavoglurant can be used for the research of Fragile X syndrome (FXS), and L-dopa induced dyskinesias in Parkinsons disease.

性状

Solid

IC50 & Target[1][2]

mGluR5 30 nM (IC50)

体外研究(In Vitro)

Mavoglurant (1 nM-10 μM; 10 min) fully antagonizes hmGluR5-mediated responses with IC50s of 110 and 30 nM in Ca- and PI-turnover assays in L(tk-) cells stably expressing mGluR5a.
Mavoglurant (0.01 nM-10 μM) displaces the binding of the allosteric binding ligand [H]-AAE327 in a concentration-dependent manner in rat brain membranes, with an IC50 of 47 nM. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Mavoglurant (0.1-10 mg/kg; a single p.o.) inhibits the stress-induced hyperthermia (SIH) in a dose-dependent manner in mice.
Mavoglurant (9.4 mg/kg; a single p.o.) exhibits moderate oral bioavailability (32%), terminal half-life (2.9 h) and C max (plasma; brain) (950 pmol/mL; 3500 pmol/g).
Mavoglurant (3.1 mg/kg; a single i.v.) exhibits terminal half-life (0.69 h), C max (plasma; brain) (3330 pmol/mL; 8400 pmol/g) and T max (≤0.08 h). has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[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.
[2]. Jacquemont AS, et, al. Epigenetic modification of the FMR1 gene in fragile X syndrome is associated with differential response to the mGluR5 antagonist AFQ056. Sci Transl Med. 2011 Jan 5;3(64):64ra1.

溶解度数据	In Vitro: DMSO : 120 mg/mL (382.91 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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