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在色谱分析、有机合成和交叉偶联反应领域已被 1 篇同行评审文献引用。
Pranoprofen 是一种非甾体抗炎试剂 (NSAID),用于角膜炎或其他眼科疾病的研究。Pranoprofen 抑制 COX1/2 酶,从而阻断花生四烯酸转化为二十烷醇,减少前列腺素的合成。
Information
Pranoprofen Pranoprofen (Pyranoprofen) is a non-steroidal COX inhibitor, used as an anti-inflammatory drug in ophthalmology.
In vitro
Pranoprofen inhibits ER stress-induced glucose regulated protein 78 (GRP78) expression, an ER-localized molecular chaperon. Pranoprofen inhibits ER stress-induced CCAAT/enhancer-binding protein homologous protein (CHOP) expression, an apoptotic transcription factor. Pranoprofen alone induces eIF2alpha phosphorylation, which is further increased by ER stress. Pranoprofen inhibits ER stress-induced X-box-binding protein 1 (XBP-1) splicing in the primary cultured glial cells. Pranoprofen (0.0625 to 1.0\u2009g/L) has poignant cytotoxicity to human corneal endothelial (HCE) cells, and the extent of its cytotoxicity is dose- and time-dependent. Pranoprofen induces plasma membrane permeability elevation, DNA fragmentation, and apoptotic body formation, proving its apoptosis inducing effect on HCE cells. Pranoprofen above 0.0625\u2009g/L has poignant cytotoxicity on HCE cells in vitro by inducing cell apoptosis, and should be carefully employed in eye clinic.
In vivo
Pranoprofen is orally administered, urinary and fecal excretions of the radioactivity within 3 days are 81.1% and 18.7% of the dose in mice, 51.5% and 39.4% in rats, 81.8% and 9.0% in guinea pigs, and 93.2% and 3.6% in rabbits, respectively. Pranoprofen is excreted in the urine exclusively in the form of pranoprofen glucuronide in rabbit. Pranoprofen, especially the R(-)-isomer, is significantly distributed in the kidney of rabbit. Pranoprofen has a preference for glucosidation rather than glucuronidation in mice at low doses in spite of having a higher capacity of glucuronidation.
Cell Data
cell lines:KIM-2, HC11, and ES
Concentrations:
Incubation Time:
Powder Purity:≥99%
H301: 吞咽会中毒