For research use only. Not for therapeutic Use.
BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC50 of 47 nM.
BMT-145027 is a compound with high MsLM stability (85% remaining), acceptable potency (EC50=47 nM), and a modest decrease in planarity (Fsp3 = 0.17). Importantly, BMT-145027 lacks inherent mGluR5 agonist activity when tested at concentrations up to 16 μM[1].
Drug-treated and control mice are shown two identical objects. After a 24-h natural forgetting period, the mice are reintroduced to a familiar object while simultaneously presented with a novel object. Since mice spend more time exploring unfamiliar objects, improved memory is measured as time spent exploring the novel object. BMT-145027 leads to a significant increase in time spent with the novel object when dosed at 30 mg/kg, with an apparent trend in novel object preference at 10 mg/kg. Satellite animals indicates a total plasma concentration of 2800 nM at 30 mg/kg[1].
| Catalog Number | I046350 |
| CAS Number | 2018282-44-3 |
| Synonyms | 3-[4-chloro-3-(trifluoromethyl)phenyl]-4-cyclopropyl-6-phenyl-2H-pyrazolo[3,4-b]pyridine-5-carbonitrile |
| Molecular Formula | C23H14ClF3N4 |
| Purity | ≥95% |
| InChI | InChI=1S/C23H14ClF3N4/c24-17-9-8-14(10-16(17)23(25,26)27)21-19-18(12-6-7-12)15(11-28)20(29-22(19)31-30-21)13-4-2-1-3-5-13/h1-5,8-10,12H,6-7H2,(H,29,30,31) |
| InChIKey | UXLUNMKSQUMWLH-UHFFFAOYSA-N |
| SMILES | C1CC1C2=C(C(=NC3=NNC(=C23)C4=CC(=C(C=C4)Cl)C(F)(F)F)C5=CC=CC=C5)C#N |
| Reference | [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. |
