Home NF-κB IκB/IKK inhibitor - Immunology & Inflammation related chemical Mesalazine (5-ASA) For research use only.

Mesalazine (5-ASA)

Synonyms: Mesalamine, 5-Aminosalicylic acid

Mesalazine (5-ASA) is a specific inhibitor of TNFα-induced IKK activity, used to treat inflammatory bowel disease.

Mesalazine (5-ASA) Chemical Structure

Mesalazine (5-ASA) Chemical Structure

CAS: 89-57-6

Selleck's Mesalazine (5-ASA) has been cited by 2 publications

Purity & Quality Control

Batch: Purity: 99.97%
99.97

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Biological Activity

Description Mesalazine (5-ASA) is a specific inhibitor of TNFα-induced IKK activity, used to treat inflammatory bowel disease.
Targets
IKK [1]
In vitro
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]
Cell Research Cell lines BVECs
Concentrations 1 mM
Incubation Time 1 h
Method

Cells were treated with indicated concentration of drug for an hour.
In Vivo
In vivo

5-ASA exerts potent antineoplastic effects that are mediated through PPARγ in an aberrant crypt mice model.
Animal Research Animal Models A/JOlaHsd mic
Dosages 200 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05992142 Recruiting Ulcerative Colitis Belgian Inflammatory Bowel Disease Research and Development (BIRD) VZW|Ferring Pharmaceuticals November 25 2022 Phase 4
NCT04499495 Completed Ulcerative Colitis Ferring Pharmaceuticals October 25 2021 --
NCT05213234 Recruiting Ulcerative Colitis Rush University Medical Center|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) July 9 2021 Not Applicable
NCT02277223 Withdrawn Ulcerative Colitis Schneider Children''s Medical Center Israel March 1 2020 Phase 3
NCT03415711 Terminated Ulcerative Colitis VSL Pharmaceuticals|Actial Farmaceutica S.r.l. April 28 2017 Not Applicable

Chemical lnformation & Solubility

Molecular Weight 153.14 Formula

C7H7NO3
CAS No. 89-57-6 SDF Download Mesalazine (5-ASA) SDF
Smiles C1=CC(=C(C=C1N)C(=O)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 31 mg/mL ( (202.42 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 31 mg/mL

Water : Insoluble


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In vivo
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