化合物FCPR03 T39341

Product Introduction
Bioactivity


英文名: FCPR03

描述: 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。

体外活性: 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].

体内活性: 在成年雄性Sprague-Dawley大鼠脑缺血再灌注后，FCPR03能够提高缺血半暗带中磷酸化AKT、GSK3β和β-catenin的水平。在大鼠经历MCAO后，FCPR03（1.25、2.5、5 mg/kg; i.p.）能减少梗塞体积并改善神经行为结果[2]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 95 mg/mL (317.40 mM)


关键字: antidepressant-like | PDE4B1 | PDE4D7 | FCPR-03 | PDE4 | neuroprotective | ischemic | AKT | GSK3β | FCPR 03 | FCPR03 | inhibit | anti-inflammatory | Phosphodiesterase (PDE) | β-catenin | Inhibitor | stroke

相关产品: (+)-Medioresinol Di-O-β-D-glucopyranoside | Vardenafil hydrochloride | Pomiferin | Enoximone | PF-05085727 | PDE5-IN-2 | Ketotifen fumarate | OR-1896 | Tadalafil | ONO-8430506

相关库: Bioactive Compounds Library Max | Antidepressant Compound Library | Inhibitor Library | Metabolism Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途