PeptideDB

BMS-984923

CAS: 1375752-78-5 F: C22H15ClN2O2 W: 374.82

BMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (Ki = 0.6 nM), exhibits g
Data collection:peptidedb@qq.com

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Bioactivity 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].
In Vivo BMS-984923 (7.5 mg/kg or 15 mg/kg, oral gavage, once) exhibits good oral bioavailability and BBB penetration[1]. Animal Model:
Name BMS-984923
CAS 1375752-78-5
Formula C22H15ClN2O2
Molar Mass 374.82
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Reference [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.