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Purity: ≥98%
Flufenamic Acid (CI-440; CN-27554) is an anti-inflammatory agent of the NSAIDs (non-steroidal anti-inflammatory agent) class. It inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. . Flufenamic acids reversibly inhibits ICl(Ca) in Xenopus oocytes with IC50 of 28 mM, elicit in response to depolarizing voltage steps, in a dose-dependent manner, with no effect on the shape of the current-voltage curve. Flufenamic acids blocks Ca2(+)-activated non-selective cation channels in inside-out patches from the basolateral membrane of rat exocrine pancreatic cells with IC50 of 10 μM.
| ln Vitro |
Cyclooxygenase (COX) is inhibited by the nonsteroidal anti-inflammatory medication flufenamic acid. Furthermore, it has the ability to control non-selective cation channels (NSC), block L-type Ca2+ channels, regulate ion channels, and modify chloride channels. K+ channel activation. A minimum of two TRP channels (C6 and A1) are activated by flufenamic acid, while numerous TRP channels (C3, C7, M2, M3, M4, M5, M7, M8, V1, V3, and V4) are inhibited [1]. CaMKKβ, a calcium/calmodulin-dependent protein kinase kinase beta, is directly stimulated by flufenamic acid to cause AMPK activation in T84 cells [2]. Moreover, Flufenamic acid (FFA; 5-50 μM) inhibits Cl- secretion that is dependent on cAMP in intact T84 cells, apical ICl-mediated by CFTR is inhibited, and Ca2+-dependent Cl- secretion is blocked in a dose-dependent manner. At 100 μM, the IC50 of FFA's Cl-secretion is approximately 10 μM, and it almost completely blocks the T84 cell monolayer. However, it has no effect on Na+-K+ ATPase or NKCC in T84 cells [3].
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| ln Vivo |
In a mouse model of Vibrio cholerae El Tor variant (EL)-induced diarrhea, flufenamic acid (50 mg/kg, ip) exhibits anti-inflammatory effects. At 20 mg/kg, it greatly reduces EL-induced intestinal secretion and breakdown of the barrier. Furthermore, in the gut of mice infected with EL, flufenamic acid stimulates AMPK activation and suppresses pro-inflammatory mediator production and NF-κB nuclear translocation [2].
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| References |
[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. [4]. Pobbati AV, et al. Targeting the Central Pocket in Human Transcription Factor TEAD as a Potential Cancer Therapeutic Strategy. Structure. 2015;23(11):2076-2086 |
| Molecular Formula |
C14H10F3NO2
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| Molecular Weight |
281.23
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| CAS # |
530-78-9
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| Related CAS # |
Flufenamic acid-d4;1185071-99-1;Flufenamic acid-13C6;1325559-30-5
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| SMILES |
FC(C1C([H])=C([H])C([H])=C(C=1[H])N([H])C1=C([H])C([H])=C([H])C([H])=C1C(=O)O[H])(F)F
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| InChi Key |
LPEPZBJOKDYZAD-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
2-((3-(trifluoromethyl)phenyl)amino)benzoic acid
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.89 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.89 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5558 mL | 17.7790 mL | 35.5581 mL | |
| 5 mM | 0.7112 mL | 3.5558 mL | 7.1116 mL | |
| 10 mM | 0.3556 mL | 1.7779 mL | 3.5558 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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