For research use only. Not for therapeutic Use.
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].
BMS-984923 (7.5 mg/kg or 15 mg/kg, oral gavage, once) exhibits good oral bioavailability and BBB penetration[1].
| Catalog Number | I045525 |
| CAS Number | 1375752-78-5 |
| Synonyms | (4R,5R)-5-(2-chlorophenyl)-4-[5-(2-phenylethynyl)pyridin-3-yl]-1,3-oxazolidin-2-one |
| Molecular Formula | C22H15ClN2O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C22H15ClN2O2/c23-19-9-5-4-8-18(19)21-20(25-22(26)27-21)17-12-16(13-24-14-17)11-10-15-6-2-1-3-7-15/h1-9,12-14,20-21H,(H,25,26)/t20-,21-/m1/s1 |
| InChIKey | IAYVUQJOKDFLAL-NHCUHLMSSA-N |
| SMILES | C1=CC=C(C=C1)C#CC2=CC(=CN=C2)C3C(OC(=O)N3)C4=CC=CC=C4Cl |
| 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. |
