Leflunomide
Leflunomide inhibits dihydroorotate dehydrogenase, preventing UMP formation and pyrimidine synthesis. Metabolites of leflunomide may inhibit various kinases such as JNK and JAK. Leflunomide is clinically used to treat rheumatoid arthritis; it exhibits immunosuppressive, antiviral, and anticancer activities. In several cellular models, leflunomide prevents apoptosis and increases viability in human cytomegalovirus (CMV)-infected cells and inhibits replication of polyomavirus BK. Additionally, leflunomide increases activity of aryl hydrocarbon receptors, inhibiting proliferation of melanoma cells.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18938072
| Cas No. |
75706-12-6 |
|---|---|
| Purity |
≥98% |
| Formula |
C12H9F3N2O2 |
| Formula Wt. |
270.21 |
| Chemical Name |
5-Methyl-N-[4-(trifluoromethyl)phenyl]-4-isoxazolecarboxamide |
| IUPAC Name |
5-methyl-N-[4-(trifluoromethyl)phenyl]-1,2-oxazole-4-carboxamide |
| Synonym |
HWA-486; Arava |
| Melting Point |
166.5°C |
| Solubility |
Soluble in DMSO or methanol. |
| Appearance |
White or off-white crystalline powder |
Qi R, Hua-Song Z, Xiao-Feng Z. Leflunomide inhibits the apoptosis of human embryonic lung fibroblasts infected by human cytomegalovirus. Eur J Med Res. 2013 Feb 1;18:3. PMID: 23369524.
ODonnell EF, Kopparapu PR, Koch DC, et al. The aryl hydrocarbon receptor mediates leflunomide-induced growth inhibition of melanoma cells. PLoS One. 2012;7(7):e40926. PMID: 22815870.
Bernhoff E, Tylden GD, Kjerpeseth LJ, et al. Leflunomide inhibition of BK virus replication in renal tubular epithelial cells. J Virol. 2010 Feb;84(4):2150-6. PMID: 19955306.
Pinto P, Dougados M. Leflunomide in clinical practice. Acta Reumatol Port. 2006 Jul-Sep;31(3):215-24. PMID: 17094333.
