CI 583

Names

[ Name ]:
CI 583

[Synonym ]:
sodium,2-(2,6-dichloro-3-methylanilino)benzoate,hydrate
Meclomen
UNII-94NJ818U2W
Lenidolor
Meclodol
Meclofenamic acid sodium salt monohydrate

Biological Activity

[Description]:

Meclofenamic acid (Meclofenamate) sodium hydrate is a non-steroidal anti-inflammatory agent. Meclofenamic acid sodium hydrate is a highly selective FTO (fat mass and obesity-associated) enzyme inhibitor. Meclofenamic acid sodium hydrate competes with FTO binding for the m(6)A-containing nucleic acid. Meclofenamic acid sodium hydrate is a non-selective gap-junction blocker. Meclofenamic acid sodium hydrate inhibits hKv2.1 and hKv1.1, with IC50 values of 56.0 and 155.9 μM, respectively[1][2][3][4].

[Related Catalog]:

Research Areas >> Inflammation/Immunology

Research Areas >> Metabolic Disease

Research Areas >> Neurological Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

Signaling Pathways >> Cytoskeleton >> Gap Junction Protein

[Target]

Human Endogenous Metabolite

[In Vitro]

Meclofenamic acid sodium hydrate (0-100 μM, 24 h) inhibits FTO demethylation in a dose-response manner[1]. Meclofenamic acid sodium hydrate inhibits enzyme cyclooxygenase, with an IC50 about 1 μM, thereby inhibiting the production of prostaglandins[2]. Meclofenamic acid sodium hydrate inhibits the release of 5-HETE and LTB4 from human neutrophils stimulated with calcium ionophore and antagonizes the response of tissues to certain prostaglandins[2]. Western Blot Analysis[1] Cell Line: HeLa cells Concentration: 0, 12.5, 25, 50, 100 μM Incubation Time: 24 h Result: Inhibited FTO demethylation in a dose-response manner, and elevates the levels of cellular m6A in mRNA by targeting FTO.

[References]

[1]. Huang Y, et al. Meclofenamic acid selectively inhibits FTO demethylation of m6A over ALKBH5. Nucleic Acids Res. 2015 Jan;43(1):373-84.

[2]. Conroy MC, et al. Pharmacology, pharmacokinetics, and therapeutic use of meclofenamate sodium. Clin J Pain. 1991;7 Suppl 1:S44-8.

[3]. Lee YT, et al. Inhibition of hKv2.1, a major human neuronal voltage-gated K+ channel, by meclofenamic acid. Eur J Pharmacol. 1999 Aug 13;378(3):349-56.

[4]. Eleftheriou CG, et al. Meclofenamic acid improves the signal to noise ratio for visual responses produced by ectopicexpression of human rod opsin. Mol Vis. 2017 Jun 16;23:334-345. eCollection 2017.