FCPR03 是一种特异性磷酸二酯酶 4 (PDE4) 抑制剂，对 PDE4B1、PDE4D7 和 PDE4 催化结构域的 IC50 分别为 31 nM、47 nM 和 60 nM。 FCPR03 具有神经保护、抗炎和抗抑郁样作用。

FCPR03 is a selective inhibitor of phosphodiesterase 4 (PDE4) with IC50s of 31 nM, 47 nM, and 60 nM for PDE4B1, PDE4D7, and PDE4 catalytic domain, respectively. FCPR03 has neuroprotective, anti-inflammatory, and antidepressant-like effects.

FCPR03 displays at least 2100-fold selectivity over other PDEs (PDE1-3 and PDE5-11). In HT-22 cells, FCPR03 (5, 10, and 20 μM) increases cell viability under the oxygen-glucose deprivation (OGD) induced condition in a dose-dependent manner. FCPR03 (20 μM) increases the levels of phosphorylated AKT, GSK-3β, and β-catenin. FCPR03 (20 μM) protects against OGD-induced cellular apoptosis in both HT-22 cells and cortical neurons. The levels of mitochondrial membrane potential (MMP) and ROS are restored by FCPR03. FCPR03 (10 μM) shows significant protective effects[2].

In adult male Sprague-Dawley rats following cerebral ischemia-reperfusion, FCPR03 increases the levels of phosphorylated AKT, GSK3β and β-catenin within the ischemic penumbra. In rats following MCAO, FCPR03 (1.25, 2.5, 5 mg/kg; i.p.) reduces the infarct volume and improves neurobehavioral outcomes[2].

1917347-65-9

C15H19F2NO3

299.318

DMSO:95 mg/mL (317.40 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years