Cat. No.: HY-B1221

Flufenamic acid

9 Cited Publications

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Based on 9 publication(s) in Google Scholar

Flufenamic acid is a non-steroidal anti-inflammatory agent, 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 acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.

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Pureté: 99.98%
CAS No.: 530-78-9
Formule: C₁₄H₁₀F₃NO₂
Masse moléculaire:281.23

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Flufenamic acid Chemical Structure

CAS No.: 530-78-9

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (9)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

L-type calcium channel

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Cellular Effect

Cell Line	Type	Value	Description	References
COS-7	EC₅₀	100 μM Compound: 14; FFA	Activation of TREK1 (unknown origin) expressed in COS7 cells assessed as increase in whole cell currents at +50 mV relative to control Activation of TREK1 (unknown origin) expressed in COS7 cells assessed as increase in whole cell currents at +50 mV relative to control	[PMID: 26588045]
CWR22R	IC₅₀	115 μM Compound: FLU	Antiproliferative activity against human 22Rv1 cells after 72 hrs by sulforhodamine B colorimetric proliferation assay Antiproliferative activity against human 22Rv1 cells after 72 hrs by sulforhodamine B colorimetric proliferation assay	[PMID: 28881288]
CWR22R	IC₅₀	115 μM Compound: FLU	Antiproliferative activity against human 22Rv1 cells after 72 hrs by sulforhodamine B colorimetric assay Antiproliferative activity against human 22Rv1 cells after 72 hrs by sulforhodamine B colorimetric assay	[PMID: 29602039]
HEK293	EC₅₀	474 μM Compound: 1	Activation of human TRESK channel expressed in HEK293 cells assessed as induction of channel current by whole cell patch clamp assay Activation of human TRESK channel expressed in HEK293 cells assessed as induction of channel current by whole cell patch clamp assay	[PMID: 27641472]
HEK293	EC₅₀	7 μM Compound: FFA	Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay	[PMID: 30878828]
LNCaP	EC₅₀	200 μM Compound: 5, flufenamic acid	Decrease in androgen receptor protein expression in LNCaP cells by Western blotting Decrease in androgen receptor protein expression in LNCaP cells by Western blotting	[PMID: 17383188]
LNCaP	IC₅₀	>50 μM Compound: 7, FLUF	Transcriptional activity at human androgen receptor BF3 site stably transfected in eGFP-expressing human LNCAP cells after 5 days by fluorometric analysis Transcriptional activity at human androgen receptor BF3 site stably transfected in eGFP-expressing human LNCAP cells after 5 days by fluorometric analysis	[PMID: 22047606]

In Vitro

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)^[1]. Flufenamic acid induces AMPK activation in T84 cells, and such an effect is via a direct stimulation of calcium/calmodulin-dependent protein kinase kinase beta (CaMKKβ) activity^[2]. Moreover, Flufenamic acid (FFA; 5-50 μM) dose-dependently inhibits cAMP-dependent Cl^- secretion in intact T84 cells, suppresses CFTR-mediated apical I_Cl^-, and blocks the Ca²⁺-dependent Cl^- secretion in a dose-dependent manner with IC₅₀ of appr 10 μM and near complete inhibition at 100 μM in T84 cell monolayers, but shows no effect on Na⁺-K⁺ ATPase or NKCC in T84 cells^[3]. Ufenamat at low concentrations can promote osteogenesis of bone marrow mesenchymal stem cells (mBMMSCs) by co-culture with mouse skin mesenchymal stem cells (mSMSCs) ^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Flufenamic acid (50 mg/kg, i.p.) has anti-inflammatory effect in a mouse model of Vibrio cholerae El Tor variant (EL)-induced diarrhea and significantly abrogates EL-induced intestinal fluid secretion and barrier disruption at 20 mg/kg. Furthermore, Flufenamic acid suppresses NF-κB nuclear translocation and expression of proinflammatory mediators and promotes AMPK phosphorylation in the EL-infected mouse intestine^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 530-78-9
Appearance Solid
Masse moléculaire 281.23
Formule C₁₄H₁₀F₃NO₂
Color White to off-white
SMILES

O=C(O)C1=CC=CC=C1NC2=CC=CC(C(F)(F)F)=C2
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (9)

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Nature

Bitter taste TAS2R14 activation by intracellular tastants and cholesterol. [Abstract]

2024 Jul;631(8020):459-466. PMID: 38776963
Adv Sci (Weinh)

Targeting Transient Receptor Potential Melastatin-2 (TRPM2) Enhances Therapeutic Efficacy of Third Generation EGFR Inhibitors against EGFR Mutant Lung Cancer. [Abstract]

2024 Sep;11(35):e2310126. PMID: 39044361
Burns Trauma

Flufenamic acid inhibits pyroptosis in ischemic flaps via the AMPK-TRPML1-Calcineurin signaling pathway. [Abstract]

2025 Feb 17:13:tkaf007. PMID: 40655077

Flufenamic acid purchased from MedChemExpress. Usage Cited in: Burns Trauma. 2025 Feb 17:13:tkaf007. [Abstract]

HE staining samples from Flufenamic acid (FFA) (12 mg/kg, i.p.) and control groups in the peri-necrotic region reveal blood vessel density.

Flufenamic acid purchased from MedChemExpress. Usage Cited in: Burns Trauma. 2025 Feb 17:13:tkaf007. [Abstract]

WB analysis of mouse flaps showing VEGF, Cadherin5, and MMP9 expression with GAPDH as the reference treated with Flufenamic acid (FFA) (12 mg/kg, i.p.).

Flufenamic acid purchased from MedChemExpress. Usage Cited in: Burns Trauma. 2025 Feb 17:13:tkaf007. [Abstract]

On Day 7 postoperatively, flaps from the stated groups were stained with CD31 and EMCN via IF treated with Flufenamic acid (FFA) (12 mg/kg, i.p.).
J Med Chem

A Novel Compound 3a-M1, from Metabolites of Sinomenine Derivative 3a, Exerts Potent Anti-Aplastic Anemia Activity via IP3R/ORAI-Mediated CTL Ferroptosis. [Abstract]

2025 Apr 17. PMID: 40243551
Antiviral Res

Seasonal coronavirus infections trigger NLRP3 inflammasome activation in macrophages but is therapeutically targetable. [Abstract]

2023 Aug:216:105674. PMID: 37459896
Microbiol Spectr

Repurposing flufenamic acid as a putative PmrB-directed adjuvant to restore colistin activity in Klebsiella pneumoniae. [Abstract]

2026 Mar 17:e0362025. PMID: 41842337
Neurosci Lett

Orexin enhances firing activities in the gigantocellular reticular nucleus through the activation of non-selective cationic conductance. [Abstract]

2020 Aug 10:733:135088. PMID: 32464262
Neurosci Lett

Fenamates inhibit human sodium channel Nav1.7 and Nav1.8. [Abstract]

2019 Mar 23:696:67-73. PMID: 30528877
bioRxiv

2024 Apr 15.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (355.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (8.89 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.89 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 3

Add each solvent one by one: 2% DMSO 40% PEG300 5% Tween-80 53% Saline

Solubility: ≥ 1.25 mg/mL (4.44 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Cell Assay^[3]

In brief, apical and basolateral chambers are filled symmetrically with Kreb's solutions. Thereafter, DMSO or Flufenamic acid is added into the basolateral chamber followed by apical membrane permealization by amphotericin B. After the amphotericin B-elicited I_sc is stabilized, ouabain is added into the basolateral chamber. The ouabain sensitive I_sc is used as an indicator of Na⁺-K⁺ ATPase activity^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]

Rats^[2]
Six-week-old male ICR outbred mice (weight 30-35 g) are fasted for 24 h before anesthesia using an intraperitoneal injection of nembutal (60 mg/kg). Following abdominal incision, the ileum is ligated (appr 3-4 cm long) and inoculated with 100 µL of PBS or PBS containing V. cholerae (10⁵ CFU/loop) with or without a concomitant intraperitoneal injection of Flufenamic acid or metformin. Twelve hours post-inoculation, ileal loops are removed for weight/length ratio measurement, biochemical analysis and ultrastructural evaluation^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (282 KB)
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Guinamard R, et al. Flufenamic acid as an ion channel modulator. Pharmacol Ther. 2013 May;138(2):272-84. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[5]. Fan Yang, et al. Topical Application of Butyl Flufenamate Ointment Promotes Cranial Defect Healing in Mice by Inducing BMP2 Secretion in Skin Mesenchymal Stem Cells. Cells. 2022 Nov 15;11(22):3620. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.5558 mL	17.7790 mL	35.5581 mL	88.8952 mL
	5 mM	0.7112 mL	3.5558 mL	7.1116 mL	17.7790 mL
	10 mM	0.3556 mL	1.7779 mL	3.5558 mL	8.8895 mL
	15 mM	0.2371 mL	1.1853 mL	2.3705 mL	5.9263 mL
	20 mM	0.1778 mL	0.8890 mL	1.7779 mL	4.4448 mL
	25 mM	0.1422 mL	0.7112 mL	1.4223 mL	3.5558 mL
	30 mM	0.1185 mL	0.5926 mL	1.1853 mL	2.9632 mL
	40 mM	0.0889 mL	0.4445 mL	0.8890 mL	2.2224 mL
	50 mM	0.0711 mL	0.3556 mL	0.7112 mL	1.7779 mL
	60 mM	0.0593 mL	0.2963 mL	0.5926 mL	1.4816 mL
	80 mM	0.0444 mL	0.2222 mL	0.4445 mL	1.1112 mL
	100 mM	0.0356 mL	0.1778 mL	0.3556 mL	0.8890 mL

Keywords

Flufenamic acid

9 Cited Publications

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Flufenamic acid

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Publications Citing Use of MedChemExpress (MCE) Flufenamic acid

Voir tous les produits spécifiques à Isoform COX

Voir tous les produits spécifiques à Isoform AMPK

Voir tous les produits spécifiques à Isoform Calcium Channel

Voir tous les produits spécifiques à Isoform Parasite

Activité biologique

Chemical Information

Publications (9)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Flufenamic acid Related Classifications

HY-B1221 Related Classifications