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2018282-44-3

中文名稱 2018282-44-3
英文名稱 BMT-145027
CAS 2018282-44-3
分子式 C23H14ClF3N4
分子量 438.83
MOL 文件 2018282-44-3.mol
更新日期 2023/03/20 15:41:21
2018282-44-3 結(jié)構(gòu)式 2018282-44-3 結(jié)構(gòu)式

基本信息

中文別名
化合物 T10573
化合物BMT-145027
英文別名
BMT-145027
BMT145027
BMT 145027
3-[4-chloro-3-(trifluoromethyl)phenyl]-4-cyclopropyl-6-phenyl-2H-pyrazolo[3,4-b]pyridine-5-carbonitrile
1H-Pyrazolo[3,4-b]pyridine-5-carbonitrile, 3-[4-chloro-3-(trifluoromethyl)phenyl]-4-cyclopropyl-6-phenyl-

物理化學(xué)性質(zhì)

沸點(diǎn)653.2±55.0 °C(Predicted)
密度1.51±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO : 2.4 mg/mL (5.47 mM)
酸度系數(shù)(pKa)7.40±0.40(Predicted)
形態(tài)Solid
顏色Light yellow to yellow

常見問題列表

生物活性
BMT-145027是 mGluR5 的正變構(gòu)調(diào)節(jié)物且沒有固有的激動(dòng)劑活性,EC50值為47 nM。
靶點(diǎn)

mGluR5

47 nM (EC 50 )

體外研究

BMT-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.

體內(nèi)研究

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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