BMT-145027 (C09-1113-398)

BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC 50 of 47 nM.In VitroBMT-145027 is a compound with high MsLM stability (85% remaining), acceptable potency (EC 50 =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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoDrug-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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:mGluR5 47 nM (EC 50 ). Specification: 0.98 Molecular Formula: C23H14ClF3N4 Molecular Weight: 438.83 PubChem CID: 129012190 Isomeric SMILES: C1CC1C2=C(C(=NC3=NNC(=C23)C4=CC(=C(C=C4)Cl)C(F)(F)F)C5=CC=CC=C5)C#N