Leflunomide

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Cat.No. 2228 - Leflunomide | C12H9F3N2O2 | CAS No. 75706-12-6
Description: Inhibitor of DHODH
Alternative Names: HWA 486, RS-34821
Chemical Name: 5-Methyl-N-[4-(trifluoromethyl)phenyl]-4-isoxazolecarboxamide
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Reviews
Literature

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
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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 27.01 100
DMSO 27.01 100

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

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References

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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View Related Products by Product Action

View all Dihydroorotate Dehydrogenase Inhibitors

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

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Multiple Sclerosis

Multiple Sclerosis Poster

Multiple sclerosis (MS) is an autoimmune disease that is characterized by focal demyelination and axon degeneration in the central nervous system. This poster summarizes the neurobiology and current therapies of MS.

Rheumatoid Arthritis

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.