Lumiracoxib
Lumiracoxib is a non-steroidal anti-inflammatory drug (NSAID) that acts as an inhibitor of COX enzymes with specificity for COX-2. Like other NSAIDs, lumiracoxib exhibits anti-inflammatory, analgesic, antipyretic, and antinociceptive activities. In animal models of metabolic syndrome, lumiracoxib reverses vascular remodeling and inflammation. In animal models with experimental autoimmune encephalitis (EAE, a translational model of multiple sclerosis), lumiracoxib inhibits lymphocyte responses and decreases disease severity; in similar in vitro models, lumiracoxib inhibits T cell proliferation and modulates expression of T-bet, IL-10, and IFN-γ. This compound may also inhibit thromboxane receptors. Additionally, lumiracoxib exhibits some anticancer potential, inducing G0/G1 cell cycle arrest and apoptosis and inhibiting proliferation in non-small cell lung cancer (NSCLC) cell lines.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18940895
| Cas No. |
220991-20-8 |
|---|---|
| Purity |
≥98% |
| Formula |
C15H13ClFNO2 |
| Formula Wt. |
293.72 |
| Chemical Name |
2-[(2-Chloro-6-fluorophenyl)amino]-5-methylbenzeneacetic acid |
| IUPAC Name |
2-[2-(2-chloro-6-fluoroanilino)-5-methylphenyl]acetic acid |
| Melting Point |
158-159°C |
| Appearance |
Pale Yellow Crystal |
Windsor MA, Valk PL, Xu S, et al. Exploring the molecular determinants of substrate-selective inhibition of cyclooxygenase-2 by lumiracoxib. Bioorg Med Chem Lett. 2013 Nov 1;23(21):5860-4. PMID: 24060487.
Renna NF, Diez ER, Lembo C, et al. Role of Cox-2 in vascular inflammation: an experimental model of metabolic syndrome. Mediators Inflamm. 2013;2013:513251. PMID: 23476105.
Hao JQ, Li Q, Xu SP, et al. Effect of lumiracoxib on proliferation and apoptosis of human nonsmall cell lung cancer cells in vitro. Chin Med J (Engl). 2008 Apr 5;121(7):602-7. PMID: 18466679.
Selg E, Buccellati C, Andersson M, et al. Antagonism of thromboxane receptors by diclofenac and lumiracoxib. Br J Pharmacol. 2007 Dec;152(8):1185-95. Erratum in: Br J Pharmacol. 2008 Apr;153(8):1763. Ambrosio, E [corrected to Ambrosio, M]. PMID: 17965743.
Ni J, Shu YY, Zhu YN, et al. COX-2 inhibitors ameliorate experimental autoimmune encephalomyelitis through modulating IFN-gamma and IL-10 production by inhibiting T-bet expression. J Neuroimmunol. 2007 May;186(1-2):94-103. PMID: 17442406.
Esser R, Berry C, Du Z, et al. Preclinical pharmacology of lumiracoxib: a novel selective inhibitor of cyclooxygenase-2. Br J Pharmacol. 2005 Feb;144(4):538-50. PMID: 15655513.
