Catalog No.S1681 Synonyms: 5-Aminosalicylic acid
Molecular Weight(MW): 153.14
Mesalamine is a specific inhibitor of TNFα-induced IKK activity, used to treat inflammatory bowel disease.
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Choose Selective IκB/IKK Inhibitors
|Description||Mesalamine is a specific inhibitor of TNFα-induced IKK activity, used to treat inflammatory bowel disease.|
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.  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.  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.  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.  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. 
-  Egan LJ, et al. J Biol Chem,?999, 274(37), 26448-26453.
-  Khare V, et al. Biochem Pharmacol,?013, 85(2), 234-244.
-  Das KK, et al. Mol Pharmacol,?009, 76(1), 183-191.
|In vitro||DMSO||31 mg/mL (202.42 mM)|
|Ethanol||31 mg/mL (202.42 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02125292||Completed||Drug: Mesalamine||Healthy||Shire||June 2014||Phase 1|
|NCT01805791||Terminated||Drug: HMPL-004 tablet|Drug: Placebo||Ulcerative Colitis||Hutchison Medipharma Limited||March 2013||Phase 3|
|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||--|
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