| 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 |
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| 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. |