BMT-145027 

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

438.83

C₂₃H₁₄ClF₃N₄

2018282-44-3

Solid

Light yellow to yellow

ClC(C(C(F)(F)F)=C1)=CC=C1C2=NNC3=NC(C4=CC=CC=C4)=C(C#N)C(C5CC5)=C32

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

• [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.  [Content Brief]