Catalog No.S1960 Synonyms: Pyranoprofen
Molecular Weight(MW): 255.27
Pranoprofen is a non-steroidal COX inhibitor, used as an anti-inflammatory drug in ophthalmology.
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|Description||Pranoprofen is a non-steroidal COX inhibitor, used as an anti-inflammatory drug in ophthalmology.|
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 g/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 g/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. |
|In vitro||DMSO||51 mg/mL (199.78 mM)|
|Ethanol||6 mg/mL (23.5 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03013959||Recruiting||Keratitis Herpetic||Peking Union Medical College||November 2016||--|
|NCT03355638||Completed||Macular Edema||Università degli Studi di Brescia||January 2016||Phase 4|
|NCT03712670||Completed||Retinal Disease||Università degli Studi di Brescia||January 1 2016||Not Applicable|
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