Naproxen 是COX 抑制剂,用于 COX-1 和 COX-2,具有镇痛和解热特性。
产品描述
Naproxen is a COX inhibitor for COX-1 and COX-2 with analgesic and antipyretic properties.
体外活性
在Carrageenan诱导关节炎的痛觉缺失大鼠模型中(IC50=27 μM)和酵母性发热大鼠模型中(IC50=40 μM), Naproxen能够产生抑制作用.在大鼠中,Naproxen能够抑制脂多糖诱导的PGE2(IC50=12.8 μM)和TXB2(IC50=5.9 μM)的产生.
体内活性
在HCA-7结肠癌细胞中(IC50=1.45 mM),高浓度的Naproxen能够诱导细胞凋亡。在细胞内,Naproxen能够抑制COX-1(IC50=2.2 μg/mL)和 COX-2(IC50=1.3 μg/mL)。
激酶实验
COX-1 and COX-2 activities in intact cells: For the determination of COX-1 and COX-2 inhibition, bovine aortic endothelial cells (BAEC) are incubated for 30 minutes with Naproxen (0.1 ng/mL to 1 mg/mL), and cultured J774.2 macrophages are treated with endotoxin at 1 μg/mL for 12 hours to induce COX-2 followed by incubated for 30 minutes with Naproxen (0.1 ng/mL to 1 mg/mL), respectively. Arachidonic acid (30 μM) is then added, and the cells are incubated for a further 15 minutes at 37 °C. The medium is then removed, and radioimmunoassay is used to measure the formation of 6-keto-PGF1α, PGE2, thromboxane B2, or PGF2α for the assessment of IC50 for COX-1 and COX-2.
细胞实验
Cells are exposed to Naproxen for 24 and 48 hours, respectively. At the end of incubation, cells are harvested by trypsinization, stained with trypan blue solution (0.04% wt/vol) and counted in a Neubauer haemocytometer chamber for the determination of cell viability.(Only for Reference)
Cas No.
26159-34-2
分子式
C14H13NaO3
分子量
252.245
别名
萘普生钠;Miranax;Naprelan;RS-3650;Anaprox
储存和溶解度
DMSO:11.9 mM
H2O:198.2 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years