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ALX-430-095-M050 50 mg 53.00 USD
ALX-430-095-G001 1 g 457.00 USD
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Immunosuppressive drug that inhibits T and B cell responses in vivo. Inhibitor of tyrosine phosphorylation (tyrosine kinase inhibitor), of dihydroorotate dehydrogenase, an enzyme for de novo pyrimidine synthesis, of TNF-dependent NF-κB activation, and of COX-2. The physiological activity of leflunomide is attributed mainly to its metabolite A77 1726 (Prod. No. ALX-430-096).

Product Specification

Alternative Name:HWA486, 5-Methylisoxazole-4-(4-trifluoromethylcarboxanilide), N-(4-Trifluoromethylphenyl)-5-methylisoxazol-4-carboxamide
MI:14: 5432
Purity:≥98.5% (HPLC)
Identity:Determined by IR.
Appearance:White to off-white crystalline powder.
Solubility:Soluble in DMSO or methanol.
Long Term Storage:+4°C
Handling:Protect from light. Keep under inert gas.
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Product Literature References

Leflunomide: mode of action in the treatment of rheumatoid arthritis: F.C. Breedveld & J.M. Dayer; Ann. Rheum. Dis. 59, 841 (2000), Abstract;
A771726, the active metabolite of leflunomide, directly inhibits the activity of cyclo-oxygenase-2 in vitro and in vivo in a substrate- sensitive manner: L.C. Hamilton, et al.; Br. J. Pharmacol. 127, 1589 (1999), Abstract;
Immunosuppressive leflunomide metabolite (A77 1726) blocks TNF- dependent nuclear factor-kappa B activation and gene expression: S.K. Manna and B.B. Aggarwal; J. Immunol. 162, 2095 (1999), Abstract;
In vivo activity of leflunomide: pharmacokinetic analyses and mechanism of immunosuppression: A.S. Chong, et al.; Transplantation 68, 100 (1999), Abstract;
Inhibition of JAK3 and STAT6 tyrosine phosphorylation by the immunosuppressive drug leflunomide leads to a block in IgG1 production: K.F. Siemasko, et al.; J. Immunol. 160, 1581 (1998), Abstract;
Leflunomide, a novel immunomodulating agent, prevents the development of allergic sensitization in an animal model of allergic asthma: E. Eber, et al.; Clin. Exp. Allergy 28, 376 (1998), Abstract;
Species-related inhibition of human and rat dihydroorotate dehydrogenase by immunosuppressive isoxazol and cinchoninic acid derivatives: W. Knecht & M. Löffler; Biochem. Pharmacol. 56, 1259 (1998), Abstract;
In vivo mechanism by which leflunomide controls lymphoproliferative and autoimmune disease in MRL/MpJ-lpr/lpr mice: X. Xu, et al.; J. Immunol. 159, 167 (1997), Abstract;
Potencies of leflunomide and HR325 as inhibitors of prostaglandin endoperoxide H synthase-1 and -2: comparison with nonsteroidal anti- inflammatory drugs: A.P. Curnock, et al.; J. Pharmacol. Exp. Ther. 282, 339 (1997), Abstract;
Molecular mechanisms of action of new xenobiotic immunosuppressive drugs: tacrolimus (FK506), sirolimus (rapamycin), mycophenolate mofetil and leflunomide: T.R. Brazelton & R.E. Morris; Curr. Opin. Immunol. 8, 710 (1996), Abstract;
Regulation of B cell function by the immunosuppressive agent leflunomide: K.F. Siemasko, et al.; Transplantation 61, 635 (1996), Abstract;
The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase: J.P. Davis, et al.; Biochemistry 35, 1270 (1996), Abstract;
Two activities of the immunosuppressive metabolite of leflunomide, A77 1726. Inhibition of pyrimidine nucleotide synthesis and protein tyrosine phosphorylation: X. Xu, et al.; Biochem. Pharmacol. 52, 527 (1996), Abstract;
Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide: X. Xu, et al.; J. Biol. Chem. 270, 12398 (1995), Abstract; Full Text
Inhibition of the epidermal growth factor receptor tyrosine kinase activity by leflunomide: T. Mattar, et al.; FEBS Lett. 334, 161 (1993), Abstract;
Leflunomide (HWA 486), a novel immunomodulating compound for the treatment of autoimmune disorders and reactions leading to transplantation rejection: R.R. Bartlett, et al.; Agents Actions 32, 10 (1991), Abstract;
Immunopharmacological profile of a novel isoxazol derivative, HWA 486, with potential antirheumatic activity-I. Disease modifying action on adjuvant arthritis of the rat: R.R. Bartlett & R. Schleyerbach; Int. J. Immunopharmacol. 7, 7 (1985), Abstract;

General Literature References

Experiences with leflunomide in solid organ transplantation: J.W. Williams, et al.; Transplantation 73, 358 (2002), (Review), Abstract;
Leflunomide and methotrexate: R.F. Laan, et al.; Curr. Opin. Rheumatol. 13, 159 (2001), (Review), Abstract;
Leflunomide, a novel immunomodulator for the treatment of active rheumatoid arthritis: M.M. Goldenberg; Clin. Ther. 21, 1837 (1999), (Review), Abstract;
Leflunomide, mycophenolic acid and matrix metalloproteinase inhibitors: D.E. Furst; Rheumatology (Oxford) 38 Suppl 2, 14 (1999), (Review), Abstract;

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A77 1726 

Dihydrorotate dehydrogenase inhibitor
108605-62-5, ≥98% (HPLC) | Print as PDF
ALX-430-096-M005 5 mg 56.00 USD
ALX-430-096-M025 25 mg 217.00 USD
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