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Inhibitor of dihydroorotate dehydrogenase (IC50 = 2.5 μM). Inhibits de novo pyrimidine synthesis in human T cells in vitro; also inhibits lymphocyte proliferation. Exhibits efficacy in several animal models of autoimmune disease, arthritis and graft rejection. Active metabolite, teriflunomide (A77 1726, Cat. No. 5069), also available.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 270.21. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.7 mL||18.5 mL||37.01 mL|
|5 mM||0.74 mL||3.7 mL||7.4 mL|
|10 mM||0.37 mL||1.85 mL||3.7 mL|
|50 mM||0.07 mL||0.37 mL||0.74 mL|
References are publications that support the biological activity of the product.
Greene et al (1995) Inhibition of dihydroorotate dehydrogenase by the immunosuppressive agent leflun. Biochem.Pharmacol. 50 861 PMID: 7575649
Cherwinski et al (1995) The immunosuppressant leflun. inhibits lymphocyte proliferation by inhibiting pyrimidine biosynthesis. J.Pharmacol.Exp.Ther. 275 1043 PMID: 7473131
Brazelton and Morris (1996) Molecular mechanisms of action of new xenobiotic immunosuppressive drugs: tacro. (FK506), siro. (rapamycin), mycophen. mofetil and leflun. Curr.Opin.Immunol. 8 710 PMID: 8902398
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Keywords: Leflunomide, Leflunomide supplier, Dihydroorotate, inhibitors, inhibits, dehydrogenases, DHOD, HWA486, immunosuppressants, HWA, 486, RS-34821, Immunosuppressants, Dihyroorotate, Dehydrogenase, DNA,, RNA, and, Protein, Synthesis, 2228, Tocris Bioscience
1 Citation for Leflunomide
Citations are publications that use Tocris products. Selected citations for Leflunomide include:
Risse et al (2011) Interleukin-13 inhibits proliferation and enhances contractility of human airway smooth muscle cells without change in contractile phenotype. J Biomol Res Ther 300 L958 PMID: 21460123
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Literature in this Area
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Rheumatoid Arthritis Poster
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.