BMT-145027

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BMT-145027 是一种 mGluR5 正变构调节剂，不具有固有的激动剂活性 (EC50 = 47 nM)。

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).(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.

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.

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.

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Neuroscience

GluR

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2018282-44-3

438.84

C23H14ClF3N4

>98% (HPLC)

In Vitro:?DMSO : 2.4 mg/mL (5.47 mM)

FC(F)(F)c1cc(ccc1Cl)-c1n[nH]c2nc(-c3ccccc3)c(C#N)c(C3CC3)c12

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(-20℃)

With Ice Pack

≥ 2 years