BMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (K i = 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.

BMS-984923 (7.5 mg/kg or 15 mg/kg, oral gavage, once) exhibits good oral bioavailability and BBB penetration[1]. Animal Model: C57Bl6J male mice[1]. Dosage: 7.5 mg/kg or 15 mg/kg (Pharmacokinetic Analysis) Administration: Oral gavage, once. Result: The plasma concentration exceeded 2 μM at 10 hr. Brain concentrations were nearly as high as plasma concentrations when measured 3 hr after a 7.5 mg/kg oral dose

1375752-78-5

C22H15ClN2O2

374.82

BMS-984923

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years