2-(3-Trifluoromethylanilino)benzoic Acid

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Chemical Structure| 530-78-9 同义名 : 氟灭酸 ;Flufenamic acid;CI-440;INF-1837;CN-27554;NSC 219007;NSC 82699;Fluphenamic Acid;FFA
CAS号 : 530-78-9
货号 : A416271
分子式 : C14H10F3NO2
纯度 : 98%
分子量 : 281.23
MDL号 : MFCD00002422
存储条件：

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(373.36 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), and also modulates ion channels, blocking chloride channels and L-type Ca2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid inhibits a wide spectrum of TRP channels, including: C3, C7, M2, M3, M4, M5, M7, M8, V1, V3, and V4 but activates at least two TRP channels (C6 and A1)[3]. Flufenamic acid (FFA) has previously been demonstrated to be a potent activator of AMP-activated protein kinase (AMPK), which is a negative regulator of NF-κB signaling. In a mouse closed loop model of EL infection, FFA treatment (20mg/kg) significantly abrogated EL-induced intestinal fluid secretion and barrier disruption. In addition, FFA suppressed NF-κB nuclear translocation and expression of proinflammatory mediators and promoted AMPK phosphorylation in the EL-infected mouse intestine. Furthermore, FFA promoted tight junction assembly and prevented interferon gamma (IFN-γ)-induced barrier disruption in an AMPK-dependent manner[4]. FFA inhibited cAMP-dependent Cl- secretion in T84 cell monolayers with IC50 of ∼8 μM. FFA inhibited Ca2+-dependent Cl- secretion with IC50 of ∼10 μM. FFA inhibited activities of Ca2+-activated Cl- channels and KCa3.1, a Ca2+-activated basolateral K+ channels, but had no effect on activities of Na+-K+-Cl- cotransporters and Na+-K+ ATPases[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03238612 Influenza A Phase 2 Recruiting October 31, 2020 Hong Kong ... 展开 >> Ivan Hung Recruiting Hong Kong, Hong Kong Contact: Ivan FN Hung, MD FRCP    852 22554049    ivanfn@gmail.com    Sub-Investigator: Kelvin To, MD FRCPath          Sub-Investigator: KY Yuen, MD FRCPath 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.56mL

0.71mL

0.36mL

17.78mL

3.56mL

1.78mL

35.56mL

7.11mL

3.56mL
参考文献

[1]White MM, Aylwin M. Niflumic and flufenamic acids are potent reversible blockers of Ca2(+)-activated Cl- channels in Xenopus oocytes. Mol Pharmacol. 1990 May;37(5):720-4.

[2]Gogelein H, Dahlem D, et al. Flufenamic acid, mefenamic acid and niflumic acid inhibit single nonselective cation channels in the rat exocrine pancreas. FEBS Lett. 1990 Jul 30;268(1):79-82.

[3]Guinamard R, Simard C, Del Negro C. Flufenamic acid as an ion channel modulator. Pharmacol Ther. 2013;138(2):272-284

[4]Pongkorpsakol P, Satitsri S, Wongkrasant P, et al. Flufenamic acid protects against intestinal fluid secretion and barrier leakage in a mouse model of Vibrio cholerae infection through NF-κB inhibition and AMPK activation. Eur J Pharmacol. 2017;798:94-104

[5]Pongkorpsakol P, Yimnual C, Chatsudthipong V, Rukachaisirikul V, Muanprasat C. Cellular mechanisms underlying the inhibitory effect of flufenamic acid on chloride secretion in human intestinal epithelial cells. J Pharmacol Sci. 2017;134(2):93-100