1. Membrane Transporter/Ion Channel Immunology/Inflammation
  2. Chloride Channel COX
  3. Niflumic acid

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.

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Niflumic acid Chemical Structure

Niflumic acid Chemical Structure

CAS No. : 4394-00-7

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Solid + Solvent
10 mM * 1 mL in DMSO
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Solid
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Niflumic acid:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Niflumic acid

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

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[1][2][3][4][5][6][7][8].

IC50 & Target

COX-2

100 nM (IC50)

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.
Molecular Weight

282.22

Formula

C13H9F3N2O2

CAS No.
Appearance

Solid

Color

Light yellow 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
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5433 mL 17.7167 mL 35.4333 mL
5 mM 0.7087 mL 3.5433 mL 7.0867 mL
View the Complete Stock Solution Preparation Table

* 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

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Niflumic acid
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