Leflunomide

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

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 27.01 100
ethanol 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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets

Safety Datasheet

References

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


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View Related Products by Product Action

View all Other Dehydrogenase Inhibitors

Keywords: Dihydroorotate inhibitors inhibits dehydrogenases DHOD HWA486 immunosuppressants HWA 486 RS-34821 Other Dehydrogenases

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


Do you know of a great paper that uses Leflunomide from Tocris? If so please let us know.

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New Product Guide (Spring/Summer 2017)

Our new product guide highlights over 130 new products added to the Tocris Bioscience range during the first half of 2017.

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