产品
编 号:F517615
分子式:C13H11NO2
分子量:213.23
产品类型
结构图
CAS No: 91-40-7
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产品详情
生物活性:
Fenamic acid (N-Phenylanthranilic acid, NPAA) is an orally active chloride channel blocker. Fenamic acid is the basic constituent of non-steroidal anti-inflammatory agents (NSAIA), and derives into mefenamic, tofenacin, flufenac acid and melofenac acid. Fenamic acid also acts as antibacterial and analgesic agent-.
体内研究:
RPA-1 is a biomarker in the detection of collecting duct injury in papillary necrosis in male rats.Fenamic acid (N-Phenylanthranilic acid, NPAA) (350-700 mg/kg/day; o.p.; 4 d, 8 d, and 15 d) causes renal papillary necrosis and increases urinary renal papillary antigen-1 (RPA-1) in rats.Fenamic acid (20 g/0.2 mL; i.p.) shows inhibitory effect against the abdominal constriction induced by acetic acid in mice.Animal Model:Male Wistar Hannover rats (8-10 weeks old; weighting 220-270 g)
Dosage:50, 350, or up to 700 mg/kg
Administration:Oral gavage; once daily; 7 days or 14 days
Result:Increased absolute paired kidney weights (13.8% at 350 mg/kg and 21.2% at 700/500 mg/kg) and relative to body weight (10.5% at 350 mg/kg/day and 20.3% at 700/500 mg/kg/day).Caused minimal papillary necrosis of tip with necrosis, hemorrhage, and inflammation of collecting ducts.
Animal Model:Male NMRI mice (weighting 20-25 g); abdominal constriction model (writhing test), induced by acetic acid
Dosage:100 g/mL, each mice injected with 20 mL
Administration:Intraperitoneal injection; once
Result:Showed anti-nociceptive activity and inhibited the abdominal constriction with the maximal inhibition of 96.3% (Mefenamic acid).
体外研究:
Fenamic acid (N-Phenylanthranilic acid, NPAA) (2.5 mM; 3 h) inhibits Cl- transportation and blocks 36C1- uptake and efflux in endothelial cells.Fenamic acid exhibits selectivity to AKR1B10 (the tumor-marker) over human AR, and inhibits AKR1B10 with IC50s of 0.76 μM (Flufenamic acid), 1.6 μM (Mefenamic acid), 9.89 μM (Meclofenamic acid), respectively.Fenamic acid (4-16 μg/mL; 72 h) inhibits 50% of Neisseria gonorrhoeae with an MIC50 value from 4 to 16 μg/mL (tolfenamic acid, flufenamic acid, and meclofenamic acid) in a low frequency of resistance. Fenamic acid (2-8 μg/mL; 8 h) reduces the expression of the porinflammatory cytokines (IL-8, IL-6 and IL-?) by infected endocervical cells without (>128 μg/mL; 24 h) inhibition towards commensal Lactobacillus spp. belonging healthy female genital microbiota.