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 Details
| Alternative Name: | HWA486, 5-Methylisoxazole-4-(4-trifluoromethylcarboxanilide), N-(4-Trifluoromethylphenyl)-5-methylisoxazol-4-carboxamide |
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| Formula: | C12H9F3N2O2 |
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| MW: | 270.2 |
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| CAS: | 75706-12-6 |
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| MI: | 14: 5432 |
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| RTECS: | NY2354200 |
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| Purity: | ≥98.5% (HPLC) |
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| Identity: | Determined by IR. |
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| Appearance: | White to off-white crystalline powder. |
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| Solubility: | Soluble in DMSO or methanol. |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | +4°C |
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| Handling: | Protect from light. Keep under inert gas. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Ginsenoside Rb1 enhances atherosclerotic plaque stability by skewing macrophages to the M2 phenotype: X. Zhang, et al.; J. Cell. Mol. Med.
22, 409 (2018),
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Mitochondrial dysfunction induced by leflunomide and its active metabolite: J. Xuan, et al.; Toxicology
396, 33 (2018),
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Full Text
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.
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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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