Cat. No.: HY-B0493

Niflumic acid

4 Cited Publications

Customer Review

Based on 4 publication(s) in Google Scholar

Niflumic acid is a calcium-activated chloride channel blocker and COX-2 inhibitor with the IC₅₀ value of 100 nM. Niflumic acid induces apoptosis through caspase-8/Bid/Bax pathway in lung cancer cells. Niflumic acide exhibits anti-tumor activity by affecting the expression of ERK1/2 and the activity of MMP2 and MMP9. Niflumic acid has orally bioactivity. Niflumic acid acts on rheumatoid arthritis.

For research use only. We do not sell to patients.

Purity: 99.61%
CAS No.: 4394-00-7
Formula: C₁₃H₉F₃N₂O₂
Molecular Weight:282.22

Storage:

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

Niflumic acid Chemical Structure

CAS No.: 4394-00-7

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

COX-2

100 nM (IC₅₀)

All COX Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Bone marrow cell	EC₅₀	>20 μM Compound: Niflumic acid	Induction of bone marrow cell differentiation isolated from ER-HOXA9 fusion protein expressed mouse harboring GFP-lysozyme assessed as upregulation of CD11b/MAC1 after 4 days by flow cytometry Induction of bone marrow cell differentiation isolated from ER-HOXA9 fusion protein expressed mouse harboring GFP-lysozyme assessed as upregulation of CD11b/MAC1 after 4 days by flow cytometry	[PMID: 27994748]
CHO	EC₅₀	30.8 μM Compound: 8	Agonist activity at C-terminal beta-galactosidase tagged human recombinant GPR35 expressed in CHO cells after 90 mins by beta-arrestin recruitment assay Agonist activity at C-terminal beta-galactosidase tagged human recombinant GPR35 expressed in CHO cells after 90 mins by beta-arrestin recruitment assay	[PMID: 23888932]
HEK293	IC₅₀	13 μM Compound: Niflumic acid	Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method	[PMID: 21030469]
HEK293	IC₅₀	53 μM Compound: Niflumic acid	Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method	[PMID: 21030469]
HEK-293T	EC₅₀	15 μM Compound: 8	Agonist activity at human GPR35 expressed in HEK293T cells at 5 uM by EYPF-based beta-arrestin-2 luciferase reporter gene assay Agonist activity at human GPR35 expressed in HEK293T cells at 5 uM by EYPF-based beta-arrestin-2 luciferase reporter gene assay	[PMID: 23888932]
HT-29	EC₅₀	1.15 μM Compound: Niflumic acid	Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay	[PMID: 24900447]
HT-29	IC₅₀	1.28 μM Compound: Niflumic acid	Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins	[PMID: 24900447]
THP-1	EC₅₀	>20 μM Compound: Niflumic acid	Induction of human THP1 cell differentiation after 4 days by flow cytometry Induction of human THP1 cell differentiation after 4 days by flow cytometry	[PMID: 27994748]
U2OS	EC₅₀	40.2 μM Compound: Niflumic acid	Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay	[PMID: 24900447]
U-937	EC₅₀	>20 μM Compound: Niflumic acid	Induction of human U937 cell differentiation after 4 days by flow cytometry Induction of human U937 cell differentiation after 4 days by flow cytometry	[PMID: 27994748]

In Vitro

Niflumic acid (100 and 200 μM; 48 h) combined with Ciglitazone (HY-W011220) exerts cytotoxic effect against A549, H460, and H1299 cells^[5].
Niflumic acid (0-300 μM; 36 h) combined with Ciglitazone induces apoptosis in A549, H460, and H1299 cells^[5].
Niflumic acid (100 μM; 30 h) combined with Ciglitazone induces activates caspase-8/Bid/Bax pathway in lung cancer cells^[5].

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

Cell Viability Assay^[5]

Cell Line:

A549, H460, and H1299 cells
Concentration:

0 μM, 100 μM,200 μM, 300 μM
Incubation Time:

48 h
Result:

Showed a marked synergistic decrease in cell viability with Ciglitazone.

Apoptosis Analysis^[5]

Cell Line:

A549, H460, and H1299 cells
Concentration:

100 μM, 200 μM
Incubation Time:

48 h
Result:

Showed a marked synergistic increase apoptosis with Ciglitazone.

Cell Viability Assay^[5]

Cell Line:

A549, H460, and H1299 cells
Concentration:

100 μM
Incubation Time:

30 h
Result:

Showed a marked synergistic increase of proteins level of caspase-8, Bid, and Bax with Ciglitazone.

In Vivo

Niflumic acid (30 mg/kg; inhalation; 2 times in 10 min) inhibits the secretory response of mucus granules in an pig asthma model ^[8].

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

Animal Model:

Pig with asthma ^[8]
Dosage:

30 mg/kg
Administration:

Inhalation
Result:

Showed significantly inhibiting the decrease in mucus area.

Chemical Information

CAS No. 4394-00-7
Appearance Solid
Molecular Weight 282.22
Formula C₁₃H₉F₃N₂O₂
Color White to yellow
SMILES

O=C(C1=CC=CN=C1NC2=CC=CC(C(F)(F)F)=C2)O
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Publications (4)

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Journal Impact Factor

Sci Adv

A worm-like nucleic acid nanostructure for gene delivery and endosomal escape via ClC3 ion exchanger. [Abstract]

2026 Mar 6;12(10):eadw0891. PMID: 41790895
Biochem Pharmacol

E3 ubiquitin ligase ITCH-mediated proteasomal degradation of WBP2 sensitizes breast cancer cells to chemotherapy through restraining AMOTL2/c-JUN axis. [Abstract]

2024 Dec 19:116720. PMID: 39709035
J Ethnopharmacol

Shenling Baizhu powder alleviates pyrotinib-induced diarrhea via CFTR-activated chloride secretion. [Abstract]

2026 Mar 25:359:121101. PMID: 41461327
Comput Struct Biotechnol J

Network Proximity-based computational pipeline identifies drug candidates for different pathological stages of Alzheimer's disease. [Abstract]

2023 Feb 24:21:1907-1920. PMID: 36936813

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (354.33 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

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

3.5433 mL

17.7167 mL

35.4333 mL

5 mM

0.7087 mL

3.5433 mL

7.0867 mL

10 mM

0.3543 mL

1.7717 mL

3.5433 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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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 (8.86 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 (8.86 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.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 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)
Handling Instructions (2659 KB)

References

[1]. Criddle, D.N., et al., Inhibitory action of niflumic acid on noradrenaline- and 5-hydroxytryptamine-induced pressor responses in the isolated mesenteric vascular bed of the rat. Br J Pharmacol, 1997. 120(5): p. 813-8. [Content Brief]

[2]. Jabeen, T., et al., Non-steroidal anti-inflammatory drugs as potent inhibitors of phospholipase A2: structure of the complex of phospholipase A2 with niflumic acid at 2.5 Angstroms resolution. Acta Crystallogr D Biol Crystallogr, 2005. 61(Pt 12): p. 1579-86. [Content Brief]

[3]. Picollo, A., et al., Mechanism of interaction of niflumic acid with heterologously expressed kidney CLC-K chloride channels. J Membr Biol, 2007. 216(2-3): p. 73-82. [Content Brief]

[4]. Yuliya V Kucherenko, et al. Niflumic Acid Affects Store-Operated Ca2+-Permeable (SOC) and Ca2+-Dependent K+ and Cl2 Ion Channels and Induces Apoptosis in K562 Cells. J Membr Biol. 2014 Jul;247(7):627-38. [Content Brief]

[5]. Byeong Mo Kim, et al. Combined treatment with the Cox-2 inhibitor niflumic acid and PPARc ligand ciglitazone induces ER stress/caspase-8-mediated apoptosis in human lung cancer cells. Cancer Lett. 2011 Jan 28;300(2):134-44. [Content Brief]

[6]. Shengqun Luo , et al. Niflumic acid exhibits anti-tumor activity in nasopharyngeal carcinoma cells through affecting the expression of ERK1/2 and the activity of MMP2 and MMP9. Int J Clin Exp Pathol [Content Brief]

[7]. I Florentin , et al. MODULATION OF IMMUNE RESPONSES IN MICE BY ORAL ADMINISTRATION OF NIFLUMIC ACID. Int J Immunopharmacol. 1989;11(2):173-83.

[8]. Mitsuko Kondo , et al. Niflumic Acid Inhibits Goblet Cell Degranulation in a Guinea Pig Asthma Model. Allergol Int. 2012 Mar;61(1):133-42. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.5433 mL	17.7167 mL	35.4333 mL	88.5834 mL
	5 mM	0.7087 mL	3.5433 mL	7.0867 mL	17.7167 mL
	10 mM	0.3543 mL	1.7717 mL	3.5433 mL	8.8583 mL
	15 mM	0.2362 mL	1.1811 mL	2.3622 mL	5.9056 mL
	20 mM	0.1772 mL	0.8858 mL	1.7717 mL	4.4292 mL
	25 mM	0.1417 mL	0.7087 mL	1.4173 mL	3.5433 mL
	30 mM	0.1181 mL	0.5906 mL	1.1811 mL	2.9528 mL
	40 mM	0.0886 mL	0.4429 mL	0.8858 mL	2.2146 mL
	50 mM	0.0709 mL	0.3543 mL	0.7087 mL	1.7717 mL
	60 mM	0.0591 mL	0.2953 mL	0.5906 mL	1.4764 mL
	80 mM	0.0443 mL	0.2215 mL	0.4429 mL	1.1073 mL
	100 mM	0.0354 mL	0.1772 mL	0.3543 mL	0.8858 mL

Keywords

Niflumic acid

4 Cited Publications

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Niflumic acid

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Publications Citing Use of MedChemExpress (MCE) Niflumic acid

All COX Isoforms

Biological Activity

Chemical Information

Publications (4)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Niflumic acid Related Classifications

Cat. No.: HY-B0493