Mesalamine

Catalog No.S1681 Synonyms: 5-Aminosalicylic acid

Mesalamine Chemical Structure

Molecular Weight(MW): 153.14

Mesalamine is a specific inhibitor of TNFα-induced IKK activity, used to treat inflammatory bowel disease.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
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Biological Activity

Description Mesalamine 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

Solubility (25°C)

In vitro DMSO 31 mg/mL (202.42 mM)
Ethanol 31 mg/mL (202.42 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 153.14
Formula

C7H7NO3

CAS No. 89-57-6
Storage powder
Synonyms 5-Aminosalicylic acid

Bio Calculators

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00514982 Withdrawn Hermanski-Pudlak Syndrome|Colitis|Cytokines|Lymphocytes|Drug Evaluation National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) August 7, 2007 Phase 2
NCT02910245 Not yet recruiting Colitis, Ulcerative Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)|ZonMw: The Netherlands Organisation for Health Research and Development October 2016 Phase 3
NCT02864979 Not yet recruiting Colorectal Neoplasms, Hereditary Nonpolyposis Rabin Medical Center August 2016 Phase 2
NCT02683733 Recruiting Ulcerative Colitis Asian Institute of Gastroenterology, India February 2016 Phase 3
NCT02522780 Recruiting Ulcerative Colitis Ferring Pharmaceuticals October 2015 Phase 3
NCT02522767 Recruiting Ulcerative Colitis Ferring Pharmaceuticals October 2015 Phase 3

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID