VU0409106

VU0409106 is a potent and selective mGlu5 negative allosteric modulator (NAM) with an IC50 of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB) [1][2].

Product Specifications

CAS Number

[1276617-62-9]

UNSPSC

12352005

Target

MGluR

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/vu0409106.html

Purity

99.76

Solubility

DMSO : 2 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CC1=CSC(NC(C2=CC(F)=CC(OC3=CN=CN=C3)=C2)=O)=N1

Molecular Formula

C15H11FN4O2S

Molecular Weight

330.34

References & Citations

[1]Felts AS, et al. Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety. Bioorg Med Chem Lett. 2013 Nov 1;23 (21) :5779-85.|[2]Morrison RD, et al. The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5. Drug Metab Dispos. 2012 Sep;40 (9) :1834-45.