439083-90-6

中文名称 BAY 607550

英文名称 BAY 60-7550

CAS 439083-90-6

分子式 C27H32N4O4

分子量 476.57

MOL 文件 439083-90-6.mol

439083-90-6 结构式

基本信息物理化学性质常见问题列表

基本信息

英文别名

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-

所属类别

生物化工：激动剂抑制剂

物理化学性质

沸点680.7±65.0 °C(Predicted)

密度1.24±0.1 g/cm3(Predicted)

储存条件-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)

酸度系数(pKa)14.54±0.20(Predicted)

形态粉末

颜色白色至浅棕色

常见问题列表

生物活性

Bay 60-7550 是有效，选择性的 PDE2 抑制剂，Ki 值为3.8 nM。

靶点

Ki: 3.8±0.2 nM (PDE2)

体外研究

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).

体内研究

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.