Fenamic acid (N-Phenylanthranilic acid, NPAA) 是一种具有口服活性的氯通道阻滞剂。Fenamic acid 是非甾体抗炎剂 (NSAIA) 的基本成分，可衍生甲芬那酸 (mefenamic)，托芬那酸 (tofenacin)，氟芬那酸 (flufenamic acid) 和 美洛芬酸 (melofenac acid)。Fenamic acid 也可作为抗菌和镇痛剂。
| 生物活性 | Fenamic acid (N-Phenylanthranilic acid, NPAA) is an orally activechloride channelblocker. 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[1]-[6]. |
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体外研究
(In Vitro) | Fenamic acid (N-Phenylanthranilic acid, NPAA) (2.5 mM; 3 h) inhibits Cl-transportation and blocks36C1-uptake and efflux in endothelial cells[1][2].
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[4].
Fenamic acid (4-16 μg/mL; 72 h) inhibits 50% ofNeisseria gonorrhoeaewith an MIC50value from 4 to 16 μg/mL (tolfenamic acid, flufenamic acid, and meclofenamic acid) in a low frequency of resistance[5].
Fenamic acid (2-8 μg/mL; 8 h) reduces the expression of the porinflammatory cytokines (IL-8, IL-6 and IL-ss) by infected endocervical cells without (>128 μg/mL; 24 h) inhibition towards commensalLactobacillusspp. belonging healthy female genital microbiota[5].
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体内研究
(In Vivo) | RPA-1 is a biomarker in the detection of collecting duct injury in papillary necrosis in male rats[3].
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[3].
Fenamic acid (20 g/0.2 mL; i.p.) shows inhibitory effect against the abdominal constriction induced by acetic acid in mice[6].
| Animal Model: | Male Wistar Hannover rats (8-10 weeks old; weighting 220-270 g)[3] | | 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[6] | | 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). |
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| 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) |
| 溶解性数据 | In Vitro: DMSO : 125 mg/mL(586.22 mM;Need ultrasonic) H2O :< 0.1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble) 配制储备液 | 1 mM | 4.6898 mL | 23.4489 mL | 46.8977 mL | | 5 mM | 0.9380 mL | 4.6898 mL | 9.3795 mL | | 10 mM | 0.4690 mL | 2.3449 mL | 4.6898 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 4.17 mg/mL (19.56 mM); Clear solution
此方案可获得 ≥ 4.17 mg/mL (19.56 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 41.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 *以上所有助溶剂都可在本网站选购。
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