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.
性状
Solid
IC50 & Target[1][2]
Chloride Channel
体外研究(In Vitro)
Fenamic acid (N-Phenylanthranilic acid, NPAA) (2.5 mM; 3 h) inhibits Cl transportation and blocks C1 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.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[1]. Mandel KG, et al. Characterization of a cyclic AMP-activated Cl-transport pathway in the apical membrane of a human colonic epithelial cell line. J Biol Chem. 1986 Jan 15. 261(2):704-12.[2]. Ueda S, et al. Chloride efflux in cyclic AMP-induced configurational change of bovine pulmonary artery endothelial cells. Circ Res. 1990 Apr. 66(4):957-67.
溶解度数据
In Vitro: DMSO : 125 mg/mL (586.22 mM; Need ultrasonic)H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)配制储备液