BMT-145027 - mGluR 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBMT-145027Cat. No.: HY-100728CAS No.: 2018282-44-3分式: CHClFN分量: 438.83作靶點: mGluR作通路: GPCR/G Protein; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 2.4 mg/mL (5.47 mM; Ne

2、ed ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.2788 mL 11.3939 mL 22.7879 mL5 mM 0.4558 mL 2.2788 mL 4.5576 mL10 mM - - -請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 BMT-145027是mGluR5 的正變構(gòu)調(diào)節(jié)物且沒有固有的激動劑活性，EC50值為47 nM。IC50 & Target IC50: 47 nM (mGlu

3、R5) 1體外研究 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 agonistactivity when tested at concentrations up to 16 M 1.1/2 Master of Small Molecules 您邊的抑制劑

4、師www.MedChemE體內(nèi)研究 Drug-treated and control mice are shown two identical objects. After a 24-h natural forgetting period, the miceare reintroduced to a familiar object while simultaneously presented with a novel object. Since mice spendmore time exploring unfamiliar objects, improved memory is measur

5、ed as time spent exploring the novelobject. BMT-145027 leads to a significant increase in time spent with the novel object when dosed at 30mg/kg, with an apparent trend in novel object preference at 10 mg/kg. Satellite animals indicates a totalplasma concentration of 2800 nM at 30 mg/kg 1.PROTOCOLKi

6、nase Assay 1 Competition binding experiments are performed using a single concentration ( 5 nM) of 3H-MethoxyPyEP inthe presence of increasing concentrations of BMT-145027. The reaction is terminated by the addition of 5 mLof ice-cold ish buffer and rapid filtration. The filter is punched into a 96

7、well flex-plate and scintillation cocktailis added to each well. The plate is allowed to soak for 8 h and then read on the micro-beta counter. IC50values are determined using non-linear regression four-parameter logistic equation 1.MCE has not independently confirmed the accuracy of these methods. T

8、hey are for reference only.Animal Mice: Mice are dosed i.p. with either vehicle or BMT-145027 at 10 and 30 mg/kg 60 min prior to the trainingAdministration 1 session and tested for recognition. Animal behavior is video recorded during both training and testing and theamount of time spent exploring t

9、he objects determined using Cleversys software 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Hill MD, et al. Development of 1H-Pyrazolo3,4-bpyridines as Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators. ACSMed Chem Lett. 2016 Oct 3;7(12):1082-1086.McePdfHeightCaution: Product has not been fully validated for med