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.
All Tocris products are intended for laboratory research use only.
|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 solvent 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 products' biological activity.
Greene et al (1995) Inhibition of dihydroorotate dehydrogenase by the immunosuppressive agent leflunomide. Biochem.Pharmacol. 50 861 PMID: 7575649
Cherwinski et al (1995) The immunosuppressant leflunomide 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: tacrolimus (FK506), sirolimus (rapamycin), mycophenolate mofetil and leflunomide. Curr.Opin.Immunol. 8 710 PMID: 8902398
If you know of a relevant reference for Leflunomide, please let us know.
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Keywords: Leflunomide, supplier, Dihydroorotate, inhibitors, inhibits, dehydrogenases, DHOD, HWA486, immunosuppressants, HWA, 486, RS-34821, Other, Dehydrogenases, Immunosuppressants, Dihyroorotate, Dehydrogenase, DNA,, RNA, and, Protein, Synthesis, Dihyroorotate, Dehydrogenase, 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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