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| | 2-Oxazolidinone, 5-(2-chlorophenyl)-4-[5-(2-phenylethynyl)-3-pyridinyl]-, (4R,5R)- Basic information |
| | 2-Oxazolidinone, 5-(2-chlorophenyl)-4-[5-(2-phenylethynyl)-3-pyridinyl]-, (4R,5R)- Chemical Properties |
| Boiling point | 619.6±55.0 °C(Predicted) | | density | 1.38±0.1 g/cm3(Predicted) | | pka | 10.61±0.60(Predicted) | | form | Solid | | color | Off-white to light yellow |
| | 2-Oxazolidinone, 5-(2-chlorophenyl)-4-[5-(2-phenylethynyl)-3-pyridinyl]-, (4R,5R)- Usage And Synthesis |
| Uses | 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: | 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 |
| | 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. DOI:10.1016/j.celrep.2017.06.023
[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. DOI:10.1016/j.bmcl.2016.07.065 |
| | 2-Oxazolidinone, 5-(2-chlorophenyl)-4-[5-(2-phenylethynyl)-3-pyridinyl]-, (4R,5R)- Preparation Products And Raw materials |
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