| Description | BMT-145027 is a positive allosteric modulator of mGluR5 without inherent agonist activity (EC50 = 47 nM). |
| In vitro | BMT-145027 lacks inherent mGluR5 agonist activity when tested at concentrations up to 16 μM. BMT-145027 exhibits high MsLM stability (85% remaining) and a modest decrease in planarity (Fsp3 = 0.17)[1]. |
| In vivo | BMT-145027 (30 mg/kg) leads to a significant increase in time spent with the novel object, with an apparent trend in novel object preference at 10 mg/kg. Satellite animals(BMT-145027: 30 mg/kg) indicates a total plasma concentration of 2800 nM[1]. |
| Target activity | mGluR5:47 nM |
| molecular weight | 438.83 |
| Molecular formula | C23H14ClF3N4 |
| CAS | 2018282-44-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 2 mg/mL (4.56 mM), Sonication and heating are recommended. |
| References | 1. Hill MD, et al. Development of 1H-Pyrazolo[3,4-b]pyridines as Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators. ACS Med Chem Lett. 2016 Oct 3;7(12):1082-1086. |