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Submit ReviewInhibitor 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.
M. Wt | 270.21 |
Formula | C12H9F3N2O2 |
Storage | Store at +4°C |
Purity | ≥99% (HPLC) |
CAS Number | 75706-12-6 |
PubChem ID | 3899 |
InChI Key | VHOGYURTWQBHIL-UHFFFAOYSA-N |
Smiles | CC1=C(C=NO1)C(=O)NC1=CC=C(C=C1)C(F)(F)F |
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.
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
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
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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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.