Mavoglurant (AFQ 056)|cas543906-09-8|DC Chemicals

Cas No.:	543906-09-8
Chemical Name:	(3aR,4S,7aR)-Octahydro-4-hydroxy-4-[2-(3-methylphenyl)ethynyl]-1H-indole-1-carboxylic acid methyl ester
Synonyms:	(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
SMILES:	CC1=CC(C#C[C@]2(O)CCC[C@]3([H])[C@@]2([H])CCN3C(OC)=O)=CC=C1
Formula:	C₁₉NO₃H₂₃
M.Wt:	313.3908
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

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]

References:

[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.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

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