AFQ056 MedChemExpress (MCE)

Product Name	Mavoglurant
Synonyms	AFQ056 AFQ 056 AFQ 056 AFQ-056 GT0I9SV4F6 GT0I9SV4F6 Mavoglurant Synonyms AFQ056 AFQ 056 AFQ 056 AFQ-056 GT0I9SV4F6 GT0I9SV4F6 Mavoglurant MAVOGLURANT SURECN989279 CHEMBL3087515 CHEMBL3087515 UNII-GT0I9SV4F6 Mavoglurant, AFQ056 (3aR,4S,7aR)-Methyl 4-hydroxy-4-(2-M-tolylethynyl)-octahydroindole-1-carboxylate (3aR,4S,7aR)-Octahydro-4-hydroxy-4-[2-(3-methylphenyl)ethynyl]-1H-indole-1-carboxylic acid methyl ester
CAS	543906-09-8
EINECS
Chemical Formula	C19H23NO3
Molecular Weight	313.39
inchi
Package	10 mM * 1 mL;1 mg;5 mg;10 mg
Price	Email to quote
Descriptions	Mavoglurant Mavoglurant MedChemExpress (MCE) HY-15257 543906-09-8 AFQ056 99.88% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions Mavoglurant Mavoglurant MedChemExpress (MCE) HY-15257 543906-09-8 AFQ056 99.88% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. Mavoglurant (AFQ056) is a potent, selective, non-competitive and orally active mGluR5 antagonist, with an IC50 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 Parkinson's disease. Mavoglurant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Mavoglurant (1 nM-10 μM 10 min) fully antagonizes hmGluR5-mediated responses with IC50s of 110 and 30 nM in Ca2+- and PI-turnover assays in L(tk-) cells stably expressing mGluR5a[1]. Mavoglurant (0.01 nM-10 μM) displaces the binding of the allosteric binding ligand [3H]-AAE327 in a concentration-dependent manner in rat brain membranes, with an IC50 of 47 nM[1]. Mavoglurant (0.1-10 mg/kg a single p.o.) inhibits the stress-induced hyperthermia (SIH) in a dose-dependent manner in mice[1]. Mavoglurant (9.4 mg/kg a single p.o.) exhibits moderate oral bioavailability (32%), terminal half-life (2.9 h) and Cmax (plasma brain) (950 pmol/mL 3500 pmol/g)[1]. Mavoglurant (3.1 mg/kg a single i.v.) exhibits terminal half-life (0.69 h), Cmax (plasma brain) (3330 pmol/mL 8400 pmol/g) and Tmax (≤0.08 h)[1]. mGluR5 30 nM (IC50) \| \| \| \| \| \| \| \| \| \| [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. [Content Brief] [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. [Content Brief] [3]. Petrov D, et, al. Mavoglurant as a treatment for Parkinson's disease. Expert Opin Investig Drugs. 2014 Aug 23(8):1165-79. [Content Brief]
Supplier Website	https://www.medchemexpress.com/Mavoglurant.html
Last Update	2025-05-21 16:50:25

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