mavoglurant

Modify Date: 2024-01-05 17:35:34

mavoglurant Structure
mavoglurant structure
Common Name mavoglurant
CAS Number 543906-09-8 Molecular Weight 313.391
Density 1.2±0.1 g/cm3 Boiling Point 476.3±45.0 °C at 760 mmHg
Molecular Formula C19H23NO3 Melting Point N/A
MSDS N/A Flash Point 241.8±28.7 °C

 Use of mavoglurant


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]

 Names

Name methyl (3aR,4S,7aR)-4-hydroxy-4-[2-(3-methylphenyl)ethynyl]-3,3a,5,6,7,7a-hexahydro-2H-indole-1-carboxylate
Synonym More Synonyms

 mavoglurant Biological Activity

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]
Related Catalog
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.

 Chemical & Physical Properties

Density 1.2±0.1 g/cm3
Boiling Point 476.3±45.0 °C at 760 mmHg
Molecular Formula C19H23NO3
Molecular Weight 313.391
Flash Point 241.8±28.7 °C
Exact Mass 313.167786
PSA 49.77000
LogP 3.51
Vapour Pressure 0.0±1.3 mmHg at 25°C
Index of Refraction 1.602
Storage condition 2-8℃

 Synonyms

Methyl (3aR,4S,7aR)-4-hydroxy-4-[(3-methylphenyl)ethynyl]octahydro-1H-indole-1-carboxylate
AFQ-056
1H-Indole-1-carboxylic acid,octahydro-4-hydroxy-4-(2-(3-methylphenyl)ethynyl)-,methyl ester,(3aR,4S,7aR)
UNII-GT0I9SV4F6
Mavoglurant [INN]
mavoglurant
1H-Indole-1-carboxylic acid, octahydro-4-hydroxy-4-[2-(3-methylphenyl)ethynyl]-, methyl ester, (3aR,4S,7aR)-
AFQ056
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