Leflunomide

Cat. No. 2228

Leflunomide C12H9F3N2O2 [75706-12-6]

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Alternative Names: HWA 486, RS-34821

Chemical Name: 5-Methyl-N-[4-(trifluoromethyl)phenyl]-4-isoxazolecarboxamide

Biological Activity

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.

Technical Data

M.Wt:
270.21
Formula:
C12H9F3N2O2
Solubility:
Soluble to 100 mM in ethanol and to 100 mM in DMSO
Purity:
>99 %
Storage:
Store at +4°C
CAS No:
75706-12-6

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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.

Cherwinski et al (1995) The immunosuppressant leflunomide inhibits lymphocyte proliferation by inhibiting pyrimidine biosynthesis. J.Pharmacol.Exp.Ther. 275 1043. PMID: 7473131.

Greene et al (1995) Inhibition of dihydroorotate dehydrogenase by the immunosuppressive agent leflunomide. Biochem.Pharmacol. 50 861. PMID: 7575649.

If you know of a relevant reference for this product please let us know.

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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Keywords: Leflunomide, supplier, Dihydroorotate, inhibitors, inhibits, dehydrogenases, DHOD, HWA486, immunosuppressants, Tocris Bioscience, Other Dehydrogenase Inhibitor products

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