| CAS NO: | 52549-17-4 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 2g | 电议 |
| 5g | 电议 |
| 10g | 电议 |
| Molecular Weight (MW) | 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) | |
| Other info | InChi Key: TVQZAMVBTVNYLA-UHFFFAOYSA-N InChi Code: InChI=1S/C15H13NO3/c1-9(15(17)18)10-4-5-13-12(7-10)8-11-3-2-6-16-14(11)19-13/h2-7,9H,8H2,1H3,(H,17,18) SMILES Code: CC(C1=CC(CC2=CC=CN=C2O3)=C3C=C1)C(O)=O |
| Synonyms | Pyranoprofen; 2-(5H-Chromeno[2,3-b]pyridin-7-yl)propanoic acid |
| 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. |
|---|---|
| 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. |
| Animal model | Mice, rats, guinea pigs, rabbits |
| Formulation & Dosage | N/A |
| References | Neurochem Int. 2009 Jan;54(1):1-6; J Pharmacobiodyn. 1990 Dec;13(12):739-44. |
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