BMS-984923

BMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (Ki = 0.6 nM), exhibits good oral bioavailability and BBB penetration. BMS-984923 potently inhibits the PrPC-mGluR5 interaction and prevents pathological Aβo signaling without affecting physiological glutamate signaling[1][2].

Product Specifications

CAS Number

[1375752-78-5]

UNSPSC

12352005

Target

MGluR

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neurodegeneration

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/bms-984923.html

Concentration

10mM

Purity

99.50

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C1O[C@H](C2=CC=CC=C2Cl)[C@@H](C3=CC(C#CC4=CC=CC=C4)=CN=C3)N1

Molecular Formula

C22H15ClN2O2

Molecular Weight

374.82

References & Citations

[1]Laura T Haas, et al. Silent Allosteric Modulation of mGluR5 Maintains Glutamate Signaling while Rescuing Alzheimer's Mouse Phenotypes. Cell Rep. 2017 Jul 5;20 (1) :76-88.|[2]Hong Huang, et al. Oxazolidinone-based allosteric modulators of mGluR5: Defining molecular switches to create a pharmacological tool box. Bioorg Med Chem Lett. 2016 Sep 1;26 (17) :4165-9.