CAS |
530-78-9 |
Chinese Name |
氟灭酸 |
English Name |
Flufenamic Acid |
Synonyms |
氟芬那酸 |
Molecular Formula |
C14H10F3NO2 |
Molecular Weight |
281.23 |
Solubility |
Soluble in DMSO ≥5mg/mL(Need ultrasonic) |
Purity |
≥98% |
Appearance |
White to off-white Solid |
Storage |
Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
EC |
EINECS 208-494-1 |
MDL |
MFCD00002422 |
SMILES |
O=C(O)C1=CC=CC=C1NC2=CC=CC(C(F)(F)F)=C2 |
InChIKey |
LPEPZBJOKDYZAD-UHFFFAOYSA-N |
InChI |
InChI=1S/C14H10F3NO2/c15-14(16,17)9-4-3-5-10(8-9)18-12-7-2-1-6-11(12)13(19)20/h1-8,18H,(H,19,20) |
PubChem CID |
3371 |
Target Point |
COX; AMPK; Potassium Channel; Chloride Channel; Calcium Channel; Parasite |
Passage |
PI3K/Akt/mTOR;Epigenetics;Immunology & Inflammation;Membrane Transporter&Ion Channel;Neuronal Signaling |
Background |
It is a non-steroidal anti-inflammatory agent that can inhibit the activity of COX, activate the activity of AMPK, regulate ion channels, block chloride channels and L-type Ca2+ channels, Regulates non-selective cation channels, activates potassium channels (K+ channels), etc. |
Biological Activity |
Flufenamic acid 是一种非甾体类抗炎剂,能够抑制 COX 的活性,激活 AMPK 的活性,调节离子通道,阻滞氯离子通道 (chloride channel) 和 L-型钙离子通道 (L-type Ca2+ channel),调节非选择性阳离子通道,激活钾离子通道 (K+ channel) 等。[1-3] |
In Vitro |
氟芬那酸是非甾体抗炎剂,抑制环加氧酶(COX),还调节离子通道,阻断氯离子通道和L型Ca2 +通道,调节非选择性阳离子通道(NSC),激活K +通道。氟芬那酸抑制广谱的TRP通道,包括:C3,C7,M2,M3,M4,M5,M7,M8,V1,V3和V4,但激活至少两个TRP通道(C6和A1)[1]。氟芬那酸在T84细胞中诱导AMPK活化,这种作用是通过直接刺激钙/钙调蛋白依赖性蛋白激酶激酶β(CaMKKβ)活性[2]。此外,氟芬那酸(FFA;5-50μM)剂量依赖性地抑制完整T84细胞中cAMP依赖性Cl-分泌,抑制CFTR介导的顶端IC1-,并以剂量依赖性方式阻断Ca2 +依赖性Cl-分泌。在T84细胞单层中,IC50约为10μM,接近完全抑制在100μM,但对T84细胞中的Na + -K + ATP酶或NKCC没有影响[3]。 |
In Vivo |
氟虫胺酸(50mg / kg,ip)在霍乱弧菌El Tor变体(EL)诱导的腹泻的小鼠模型中具有抗炎作用,并且在20mg / kg时显着消除EL诱导的肠液分泌和屏障破坏。此外,氟芬那酸抑制NF-κB核转位和促炎介质的表达,并促进EL感染的小鼠肠中的AMPK磷酸化[2]。 |
Cell Experiment |
简而言之,顶端和基底外侧腔室用Kreb溶液对称填充。此后,将DMSO或氟芬那酸加入基底外侧室中,然后通过两性霉素B进行顶膜渗透。在两性霉素B诱发的Isc稳定后,将哇巴因加入基底外侧室中。哇巴因敏感的Isc用作Na + -K + ATP酶活性的指标[3]。 |
Animal Experiment |
大鼠[2]使用腹膜内注射戊巴比妥(60mg / kg),在麻醉前将6周龄雄性ICR远交小鼠(体重30-35g)禁食24小时。腹部切口后,连接回肠(约3-4cm长),并接种100μL含有霍乱弧菌(105CFU /环)的PBS或PBS,同时或不同时腹膜内注射氟芬那酸或二甲双胍。接种后12小时,取出回肠环进行重量/长度比测量,生化分析和超微结构评估[2]。 |
Data Literature Source |
[1]. Guinamard R,et al. Flufenamic acid as an ion channel modulator. Pharmacol Ther. 2013 May;138(2):272-84. [2]. Pongkorpsakol 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 Mar 5;798:94-104. [3]. Pongkorpsakol P,et al. Cellular mechanisms underlying the inhibitory effect of flufenamic acid on chloride secretion in human intestinal epithelial cells. J Pharmacol Sci. 2017 Jun;134(2):93-100. |
Unit |
Bottle |
Specification |
50mg 100mg 200mg |