"目錄號(hào): HY-15257A

GPCR/G Protein-

Mavoglurant racemate 是 mavoglurant 的外消旋體。Mavoglurant 是一種新穎的，非競(jìng)爭(zhēng)性的 mGlu5 受體拮抗劑。

mGluR

相關(guān)產(chǎn)品

CTEP-LY341495-LY354740-LY404039-RG7090-Mavoglurant-MPEP Hydrochloride-Dipraglurant-Topiramate-JNJ-40411813-L-Glutamine-FITM-JNJ16259685-MTEP hydrochloride-(S)-MCPG-

生物活性

Description

Mavoglurant (racemate) is the racemate of mavoglurant. Mavoglurant is a novel, non-competitive mGlu5 receptor antagonist.

In Vitro

For antagonistic activity, (?)-mavoglurant, the (?)-enantiomer shows IC50of 0.11 μM and 0.03 μM (Ca2+and PI-turnover) whereas the (+)-enantiomer ((+)-10) shows only 37% and 18% inhibition at 10 μM[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):5790-803