Molecular Formula | C27H32N4O4 |
Molar Mass | 476.57 |
Density | 1.24±0.1 g/cm3(Predicted) |
Boling Point | 680.7±65.0 °C(Predicted) |
Appearance | powder |
Color | white to light brown |
pKa | 14.54±0.20(Predicted) |
Storage Condition | -20°C |
In vitro study | 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). |
In vivo study | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.098 ml | 10.492 ml | 20.983 ml |
5 mM | 0.42 ml | 2.098 ml | 4.197 ml |
10 mM | 0.21 ml | 1.049 ml | 2.098 ml |
5 mM | 0.042 ml | 0.21 ml | 0.42 ml |
biological activity | Bay 60-7550 is an effective and selective PDE2 inhibitor with a Ki value of 3.8 nM. |
target | Ki: 3.8±0.2 nM (PDE2) |
in vitro study | 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 μ M) results in further increases in cGMP compared with NMDA alone. The NMDA receptor antagonist MK-801 (10 μ M) 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). |
in vivo study | 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 span head-dipping, compared with vehicle-treated mice; significant increases are observed at doses of 1 and 3 mg/kg. |