Description | BMS-984923 is an orally available and blood-brain barrier permeable mGluR5 silencing allosteric modulator that inhibits β-amyloid oligomer-induced aberrant synaptic signaling, and can be used to study Alzheimer's disease. |
In vivo | BMS-984923(7.5 mg/kg 或 15 mg/kg,口服管饲,一次)表现出良好的口服生物利用度和 BBB 渗透性 ;C57Bl6J 雄性小鼠 ()7.5 mg/kg 或 15 mg/kg,口服管饲,一次);导致血浆浓度在 10 小时时超过 2 μM。7.5 mg/kg 口服剂量 3 小时后测量时,脑浓度几乎与血浆浓度一样高[1]。 |
Synonyms | BMS984923, BMS 984923 |
molecular weight | 374.82 |
Molecular formula | C22H15ClN2O2 |
CAS | 1375752-78-5 |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
Solubility | DMSO: 30 mg/mL (80.04 mM), Sonication is recommended. |
References | 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. |