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Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Chemical Structure| 4394-00-7 Chemical Structure| 4394-00-7

Structure of Niflumic Acid
CAS No.: 4394-00-7

Chemical Structure| 4394-00-7

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Niflumic acid, a Ca2+-activated Cl- channel blocker, is an analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis.

Synonyms: Actol; Nifluril; Niflumic Acid, Donalgin, Flunir, Niflactol, Niflugel, Nifluril

4.5 *For Research Use Only !

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Product Details of Niflumic Acid

CAS No. :4394-00-7
Formula : C13H9F3N2O2
M.W : 282.22
SMILES Code : C1=C(C(=NC=C1)NC2=CC(=CC=C2)C(F)(F)F)C(O)=O
Synonyms :
Actol; Nifluril; Niflumic Acid, Donalgin, Flunir, Niflactol, Niflugel, Nifluril
MDL No. :MFCD00010569
InChI Key :JZFPYUNJRRFVQU-UHFFFAOYSA-N
Pubchem ID :4488

Safety of Niflumic Acid

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H301+H311+H331-H315-H319
Precautionary Statements:P501-P261-P270-P271-P264-P280-P337+P313-P305+P351+P338-P361+P364-P332+P313-P301+P310+P330-P302+P352+P312-P304+P340+P311-P403+P233-P405
Class:6.1
UN#:2811
Packing Group:

Isoform Comparison

Biological Activity

Target
  • COX-2

  • GABA receptor

In Vitro:

Cell Line
Concentration Treated Time Description References
Rat aortic smooth muscle cells 10 µM 10 min Niflumic acid did not inhibit contractions induced by KCl (up to 120 mM), which were completely blocked by nifedipine. Br J Pharmacol. 1996 Jun;118(4):1065-71
CHO cells 30, 100 µM 10 s Niflumic acid inhibited glycine-induced currents mediated by α3 glycine receptors, with higher blocking potency at positive membrane potentials. Front Mol Neurosci. 2017 May 16;10:125
CHO cells 10, 30, 100 µM 10 s Niflumic acid showed stronger inhibition of glycine-induced currents mediated by α2 glycine receptors, with pronounced voltage dependence. Front Mol Neurosci. 2017 May 16;10:125
CHO cells 30, 100, 300 µM 10 s Niflumic acid inhibited glycine-induced currents mediated by α1 glycine receptors in a voltage-dependent manner, with higher blocking potency at positive membrane potentials. Front Mol Neurosci. 2017 May 16;10:125
Rat skeletal muscle fibers 42 µM (IC50) 10–15 minutes Niflumic acid inhibits chloride conductance of rat skeletal muscle by directly inhibiting the CLC-1 channel and by increasing intracellular calcium. Br J Pharmacol. 2007 Jan;150(2):235-47
Hypoglossal motoneurons (HMs) in brainstem slices from mice 100 µM 1-3 minutes NFA inhibited the amplitude and frequency of glycinergic synaptic currents, with stronger inhibition in the neonatal group Front Mol Neurosci. 2018 Nov 13;11:416
Rat aortic smooth muscle cells 10 µM 15 min In Ca-free conditions, niflumic acid did not inhibit the transient contraction induced by 1 μM NA, indicating it does not reduce calcium release from intracellular stores or the sensitivity of the contractile apparatus to calcium. Br J Pharmacol. 1996 Jun;118(4):1065-71
Rat aortic smooth muscle cells 10 µM 15 min Niflumic acid inhibited contractions induced by brief application of 1 μM NA by 55%. Br J Pharmacol. 1996 Jun;118(4):1065-71
Rat mesenteric vascular bed smooth muscle cells 10 and 30 µM 15 minutes Niflumic acid inhibited noradrenaline- and 5-HT-induced pressor responses, with 30 μM niflumic acid reducing the pressor response to 1 nmol noradrenaline by 34±6%. Br J Pharmacol. 1997 Mar;120(5):813-8
Rat stomach fundus smooth muscle cells 1-30 µM 15 minutes Niflumic acid concentration-dependently inhibited 5-HT-induced contractions, reducing to 15.5±6.0% of control at 30 μM. Br J Pharmacol. 2000 Jun;130(3):678-84
Rat pulmonary artery smooth muscle cells 50 µM 2 minutes NFA significantly increased basal [Ca2+]i and attenuated the caffeine-induced increase in [Ca2+]i. Br J Pharmacol. 2003 Dec;140(8):1442-50
Xenopus oocytes 100 µM 2 to 5 min NFA increased Kv1.1 current amplitudes by enhancing the channel open probability, causing a hyperpolarizing shift in the voltage dependence of both channel opening and gating charge movement, slowing the OFF-gating current decay. Proc Natl Acad Sci U S A. 2023 Aug;120(31):e2207978120
HEK293 cells 50 µM 24 hours Niflumic acid (NFA) acted as a pharmacological chaperone, restoring chloride current density of A531V and V947E mutants to levels similar to WT without altering voltage dependence. Front Pharmacol. 2022 Aug 11;13:958196
Rat aortic smooth muscle cells 3 µM and 10 µM 30 min Niflumic acid reversibly and concentration-dependently inhibited noradrenaline (NA)-induced contractions, with 10 μM niflumic acid inhibiting the maximal contraction by 38%. Br J Pharmacol. 1996 Jun;118(4):1065-71
BALB/3T3 clone A31 (mouse normal fibroblasts) 158.8 ± 33.0 µM (IC50) 72 hours Evaluation of antiproliferative activity of niflumic acid alone, IC50 value was 158.8 ± 33.0 µM Int J Mol Sci. 2024 Oct 13;25(20):11015
A172 (glioblastoma) 143.2 ± 6.5 µM (IC50) 72 hours Evaluation of antiproliferative activity of niflumic acid alone, IC50 value was 143.2 ± 6.5 µM Int J Mol Sci. 2024 Oct 13;25(20):11015
MCC13 (Merkel cell cancer) 175.4 ± 6.9 µM (IC50) 72 hours Evaluation of antiproliferative activity of niflumic acid alone, IC50 value was 175.4 ± 6.9 µM Int J Mol Sci. 2024 Oct 13;25(20):11015
SK-MEL-3 (melanoma) 167.1 ± 4.4 µM (IC50) 72 hours Evaluation of antiproliferative activity of niflumic acid alone, IC50 value was 167.1 ± 4.4 µM Int J Mol Sci. 2024 Oct 13;25(20):11015
UM-SCC-17A (head and neck squamous carcinoma) 310.3 ± 32.6 µM (IC50) 72 hours Evaluation of antiproliferative activity of niflumic acid alone, IC50 value was 310.3 ± 32.6 µM Int J Mol Sci. 2024 Oct 13;25(20):11015
A-431 (epidermoid carcinoma) 153.3 ± 43.1 µM (IC50) 72 hours Evaluation of antiproliferative activity of niflumic acid alone, IC50 value was 153.3 ± 43.1 µM Int J Mol Sci. 2024 Oct 13;25(20):11015
5637 (urinary bladder carcinoma) 103.5 ± 17.1 µM (IC50) 72 hours Evaluation of antiproliferative activity of niflumic acid alone, IC50 value was 103.5 ± 17.1 µM Int J Mol Sci. 2024 Oct 13;25(20):11015

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rat Isolated mesenteric vascular bed Perfusion 10 and 30 μM 15 minutes pre-exposure Niflumic acid selectively inhibited noradrenaline- and 5-HT-induced pressor responses but did not affect KCl-induced pressor responses. Br J Pharmacol. 1997 Mar;120(5):813-8
Mice Kv1.1V408A/+ mouse model Intraperitoneal injection 10 mg/kg Single administration NFA ameliorated the motor performance of Kv1.1V408A/+ mice, significantly reducing foot slips and missteps on both narrow beam and horizontal ladder tasks. Proc Natl Acad Sci U S A. 2023 Aug;120(31):e2207978120
Mice Kir6.2−/− mice Pancreas perfusion 100 µM Single administration Niflumic acid almost completely blocked cAMP-induced glucose-stimulated insulin secretion Diabetologia. 2009 May;52(5):863-72
Rats Chronic hypoxia model Lung perfusion 30 μM Single administration To evaluate the role of Cl? channels in NS1619-induced pulmonary vasodilation Lung. 2014 Oct;192(5):811-7
Zebrafish Zebrafish embryos Bath application 500 µM 30 minutes Niflumic acid treatment caused bilateral muscle contractions in response to tactile stimulation Sci Rep. 2020 Aug 19;10(1):13999
Sprague Dawley rats Steroid-induced Pneumocystis pneumonia model Intraperitoneal injection 6 mg/kg/day Once daily for 4 weeks NFA caused a significant decrease in total mucus, MUC5AC and mCLCA3 and also, in Pneumocystis-associated inflammation. Most relevant, NFA treatment improved survival at 8 weeks of steroids. Front Microbiol. 2019 Jul 5;10:1522

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.54mL

0.71mL

0.35mL

17.72mL

3.54mL

1.77mL

35.43mL

7.09mL

3.54mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

Historical Records

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