product name Pranoprofen
Description: Pranoprofen (also known as Pyranoprofen) is a potent non-steroidal (NSAIDs) COX inhibitor that is used as an anti-inflammatory drug in ophthalmology. It inhibits ER stress-induced glucose regulated protein 78 (GRP78) expression, an ER-localized molecular chaperon. Pranoprofen also inhibits ER stress-induced CCAAT/enhancer-binding protein homologous protein (CHOP) expression, an apoptotic transcription factor.
References: Neurochem Int. 2009 Jan;54(1):1-6; J Pharmacobiodyn. 1990 Dec;13(12):739-44.
255.27
Formula
C15H13NO3
CAS No.
52549-17-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 51 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: 6 mg/mL (23.5 mM)
Solubility (In vivo)
Synonyms
Pyranoprofen
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19407733,18441629,15812270
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
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| 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. |
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| Formulation & Dosage | |
| References | Neurochem Int. 2009 Jan;54(1):1-6; J Pharmacobiodyn. 1990 Dec;13(12):739-44. |
