Mesalamine (5-ASA)

Catalog No.S1681 Synonyms: 5-Aminosalicylic acid, Mesalazine, Apriso, Asacol, Pentasa, Canasa

For research use only.

Mesalamine (5-Aminosalicylic acid, 5-ASA, Mesalazine, Apriso, Asacol, Pentasa, Canasa) is a specific inhibitor of TNFα-induced IKK activity, used to treat inflammatory bowel disease.

Mesalamine (5-ASA) Chemical Structure

CAS No. 89-57-6

Selleck's Mesalamine (5-ASA) has been cited by 2 Publications

Purity & Quality Control

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Biological Activity

Description Mesalamine (5-Aminosalicylic acid, 5-ASA, Mesalazine, Apriso, Asacol, Pentasa, Canasa) is a specific inhibitor of TNFα-induced IKK activity, used to treat inflammatory bowel disease.
Targets
IKK [1]
In vitro

Mesalamine inhibits the enzyme 3-hydroxysteroid dehydrogenase, involved in the reversible conversion between DHP and THP, and therefore may affect the local actions of DHP and THP in the brain. Mesalamine, an anti-inflammatory aminosalicylate, dose-dependently inhibits IL-1-stimulated NF-kappaB-dependent transcription without preventing IkappaB degradation or nuclear translocation and DNA binding of the transcriptionally active NF-kappaB proteins, RelA, c-Rel, or RelB. Mesalamine is found to inhibit IL-1-stimulated RelA phosphorylation. [1] Mesalamine increases cell adhesion which is measured by cell adhesion assay and transcellular-resistance measurement. Mesalamine treatment restores membranous expression of adhesion molecules E-cadherin and β-catenin. [2] Mesalamine or sulfasalazine (2 mM), but not sulfapyridine, significantly reduces the expression of the TC22 transcript and significantly reduces the expression of TC22 protein in a dose-dependent and reversible manner. [3] Mesalamine induces membranous expression of E-cadherin and increases intercellular adhesion. Mesalamine activity modulates E-cadherin glycosylation and increases both mRNA and protein levels of GnT-III and its activity as detected by increased E4-lectin reactivity. [4] Mesalamine (0.1-1 mM) shows considerable inhibition of peroxynitrite-mediated luminol chemiluminescence in a dose-dependent fashion, suggesting that Mesalamine is able to directly scavenge the peroxynitrite. Mesalamine only at higher concentration (1 mM) inhibits the hydroxyl radical adduct while shifting Electron paramagnetic resonance (EPR) spectra. [5]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 153.14
Formula

C7H7NO3

CAS No. 89-57-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC(=C(C=C1N)C(=O)O)O

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02125292 Completed Drug: Mesalamine Healthy Shire|Takeda June 2 2014 Phase 1
NCT01678300 Completed -- Ulcerative Colitis Beth Israel Deaconess Medical Center August 2012 --
NCT01349504 Completed -- Ulcerative Colitis|Crohn''s Disease Beth Israel Deaconess Medical Center|Shire April 2011 --
NCT01130844 Completed Drug: MMX Mesalamine Ulcerative Colitis Shire|Takeda October 8 2010 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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