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Niflumic acid

Catalog No. T0693 CAS 4394-00-7

Synonyms: Nifluril, Forenol, Landruma

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

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Niflumic acid, CAS 4394-00-7

Pack Size	Availability	Price/USD
50 mg	In stock	$ 44.00
100 mg	In stock	$ 54.00
200 mg	In stock	$ 75.00
500 mg	In stock	$ 119.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.79%

Biological Description

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Description

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

In vivo

Niflumic acid suppresses calcium-activated currents on the basolateral membrane of rat pancreatic exocrine cells with an IC50 of 50 μM. It dose-dependently and reversibly activates the calcium-activated potassium (KCa) channels. Niflumic acid induces a spontaneous transient concentration-dependent inhibition of inward currents (STIC, calcium-activated chloride currents) amplitude. It inhibits calcium-activated chloride channels with a Ki of 17 mM. Additionally, Niflumic acid suppresses ICl(Ca) under the permeabilizing effect of Ca2+ on oocytes through Ca2+ ionophore A23187, suggesting the inhibition of ICl(Ca) results from direct interaction with Cl- channels, not by disruption of Ca2+ entry through voltage-dependent Ca2+ channels. Niflumic acid attenuates norepinephrine and caffeine-induced inward currents (IO(Ca)) with an IC50 of 6.6 μM, which is less effective than that on spontaneous currents. It exhibits a voltage-dependent inhibition of the amplitude of spontaneous transient currents (STIC), with IC50 values of 1.1 μM at +50 mV and 2.3 μM at -50 mV. Furthermore, Niflumic acid reduces airway hyperresponsiveness and eosinophilic infiltration, as well as inhibits IL-13 induced goblet cell hyperplasia. Following the IL-13 challenge, Niflumic acid hampers the overexpression of the MUC5AC gene (a marker of goblet cell proliferation) and levels of chemokines in bronchoalveolar lavage fluid. It also represses the activation of JAK/STAT6, AK2, and the expression of chemokines in epithelial cells.

Synonyms	Nifluril, Forenol, Landruma
Molecular Weight	282.22
Formula	C13H9F3N2O2
CAS No.	4394-00-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 52 mg/mL (184.3 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. White MM, et al. Mol Pharmacol, 1990, 37(5), 720-724. 2. Goelein H, et al. FEBS Lett, 1990, 268(1), 79-82. 3. Ottolia M, et al. Biophys J, 1994, 67(6), 2272-2279. 4. Hogg RC, et al. Br J Pharmacol, 1994, 112(3), 977-984. 5. Kuang Y, Chai Y, Xu L, et al. Glabrone as a specific UGT1A9 probe substrate and its application in discovering the inhibitor glycycoumarin[J]. European Journal of Pharmaceutical Sciences. 2021: 105786.

Citations

1. Kuang Y, Chai Y, Xu L, et al. Glabrone as a specific UGT1A9 probe substrate and its application in discovering the inhibitor glycycoumarin. European Journal of Pharmaceutical Sciences. 2021: 105786.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Approved Drug Library Anti-Neurodegenerative Disease Compound Library Membrane Protein-targeted Compound Library Inhibitor Library Anti-Cancer Drug Library Drug Repurposing Compound Library Bioactive Lipid Compound Library Metabolism Compound Library Anti-Metabolism Disease Compound Library Drug-Fragment Library

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Keywords

Niflumic acid 4394-00-7 Immunology/Inflammation Membrane transporter/Ion channel Metabolism Neuroscience Others COX Chloride channel Phospholipase UGT Monocarboxylate transporter Cl? Channels Inhibitor inhibit Nifluril Chloride Channel Forenol Landruma inhibitor

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