FCPR03 是一种有效的选择性的磷酸二酯酶 4 (PDE4) 抑制剂，对于 PDE4 催化域，PDE4B1 和 PDE4D7，IC50 值分别为 60 nM，31 nM 和 47 nM。FCPR03 对 PDE4 的选择性比其他 PDE (PDE1-3 和 PDE5-11) 至少高 2100 倍。FCPR03 具有抗炎，神经保护和抗抑郁样作用。
货号:ajcx39060
CAS:1917347-65-9
分子式:C15H19F2NO3
分子量：299.31
溶解度:DMSO : 100 mg/mL (334.10 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

FCPR03 is a potent and selective phosphodiesterase 4 (PDE4) inhibitor with IC50 values of 60 nM, 31 nM and 47 nM for PDE4 catalytic domain, PDE4B1 and PDE4D7, respectively. FCPR03 displays at least 2100-fold selectivity over other PDEs (PDE1-3 and PDE5-11). FCPR03 has anti-inflammatory, neuroprotective and antidepressant-like effects[1][2].

FCPR03 (5-20 μM; 30 hours; HT-22 cells) treatment increases cell viability (oxygen-glucose deprivation (OGD)-induced) in a dose-dependent manner, and 10 μM FCPR03 shows significant protective effects[1].FCPR03 (20 μM; 30 hours; HT-22 cells) treatment protects against OGD-induced cellular apoptosis in both HT-22 cells and cortical neurons. The levels of mitochondrial membrane potential (MMP) and ROS are also restored by FCPR03[1].FCPR03 (20 μM; 30 hours; HT-22 cells) treatment increases the levels of phosphorylated AKT, glycogen synthase kinase-3β (GSK3β), and β-catenin[1].

FCPR03 (1.25-5 mg/kg; intraperitoneal injection; once; adult male Sprague-Dawley rats) treatment reduces the infarct volume and improves neurobehavioral outcomes in rats following MCAO. FCPR03 increases the levels of phosphorylated AKT, GSK3β and β-catenin within the ischemic penumbra of rats following cerebral ischemia-reperfusion[1].

[1]. Bingtian Xu, et al. FCPR03, a Novel Phosphodiesterase 4 Inhibitor, Alleviates Cerebral ischemia/reperfusion Injury Through Activation of the AKT/GSK3β/ β-catenin Signaling Pathway. Biochem Pharmacol. 2019 May;163:234-249.
[2]. Zheng-Qiang Zou, et al. Novel Phosphodiesterase 4 Inhibitor FCPR03 Alleviates Lipopolysaccharide-Induced Neuroinflammation by Regulation of the cAMP/PKA/CREB Signaling Pathway and NF- κ B Inhibition. J Pharmacol Exp Ther. 2017 Jul;362(1):67-77.

Protocol:

PDE4catalyticdomain 60nM(IC50)

PDE4B1 31nM(IC50)

PDE4D7 47nM(IC50)