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439083-90-6

中文名稱 BAY 607550
英文名稱 BAY 60-7550
CAS 439083-90-6
分子式 C27H32N4O4
分子量 476.57
MOL 文件 439083-90-6.mol
更新日期 2024/11/15 18:20:32
439083-90-6 結(jié)構(gòu)式 439083-90-6 結(jié)構(gòu)式

基本信息

英文別名
BAY 60-7550
2-(3,4-Dimethoxybenzyl)-7-((2R,3R)-2-hydroxy-6-phenylhexan-3-yl)-5-methylimidazo[5,1-f][1,2,4]
2-[(3,4-Dimethoxyphenyl)methyl]-7-[(1R)-1-[(1R)-1-hydroxyethyl]-4-phenylbutyl]-5-methyl-imidazo[5,1-f][1,2,4]triazin-4(1H)-one
Imidazo[5,1-f][1,2,4]triazin-4(1H)-one, 2-[(3,4-dimethoxyphenyl)methyl]-7-[(1R)-1-[(1R)-1-hydroxyethyl]-4-phenylbutyl]-5-methyl-
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

沸點680.7±65.0 °C(Predicted)
密度1.24±0.1 g/cm3(Predicted)
儲存條件-20°C
溶解度DMSO:21.65(Max Conc. mg/mL);45.43(Max Conc. mM)
Ethanol:10.0(Max Conc. mg/mL);20.98(Max Conc. mM)
酸度系數(shù)(pKa)14.54±0.20(Predicted)
形態(tài)粉末
顏色白色至淺棕色

常見問題列表

生物活性
Bay 60-7550 是有效,選擇性的 PDE2 抑制劑,Ki 值為3.8 nM。
靶點

Ki: 3.8±0.2 nM (PDE2)

體外研究

Bay 60-7550 (1 μM) increases cGMP in the neuronal cultures compared with control [F(6,14)=12.97, p<0.05 for Bay 60-7550]. Bay 60-7550 in the presence of NMDA (30 μM) results in further increases in cGMP compared with NMDA alone. The NMDA receptor antagonist MK-801 (10 μM) blocks both Bay 60-7550+NMDA-induced elevation in cGMP in neuronal cultures. Compared with untreated control cells, proliferation of PASMCs from IPAH patients is significantly reduced by BAY 60-7550 (1 μM).

體內(nèi)研究

The PDE2 inhibitors Bay 60-7550 (1 mg/kg) reverses restraint stress-induced alterations in behavior, resulting in increased percentages of open-arm entries and open-arm time compared with the vehicle + restraint stress condition. In nonstressed mice, Bay 60-7550 produces a dose-dependent increase in percentages of open-arm entries and open-arm time compared with the vehicle-treated group; significant increases are observed at a dose of 3 mg/kg. In nonstressed mice, Bay 60-7550 increases, in a dose-dependent manner, the number of head-dips and time spent head-dipping, compared with vehicle-treated mice; significant increases are observed at doses of 1 and 3 mg/kg.

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