Leflunomide [75706-12-6]

Cat# VD-OEIA-0113-5mg

Size : 5mg

Brand : VDM Biochemicals

Contact local distributor :


Phone : +1 850 650 7790

Product Specification

  • Appearance
    :

    White crystalline solid

  • CAS Number
    :

    75706-12-6

  • Cat.number
    :

    VD-OEIA-0113

  • Formula
    :

    C12H9F3N2O2

  • MW
    :

    270.21

  • Purity
    :

    >=99%

  • Solubility
    :

    DMSO or EtOH

  • Storage
    :

    +4°C.

  • Synonyms
    :

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

  • Size
    :

    50mg, 5mg

SKU: VD-OEIA-0113 Categories: Enzyme Inhibitors, Other Enzyme Inhibitors and Activators

Description

An immunosuppressive agent. Inhibits T and B cell proliferation. Activity is attributed mainly to its metabolite, a malononitrile derivative, which is beleived to inhibit dihydroorotate dehydrogenase as well as several protein tyrosine kinases. Therapeutically as a antirheumatic. In vitro the active metabolite A77 1726 (RS-61980) inhibits dihydroorotate dehydrogenase (Ki = 2.7 μM) and de novo pyrimidine synthesis in T-cells; blocks lymphocyte cell cycle progression and proliferation. A77 1726 also inhibits anti-CD3/CD28-induced cytokine production in PBMC cells (IC50 = 21-27 μg/ml). In vivo reduces inflammation in several animal models of autoimmune disease, arthritis, asthma and graft rejection.

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5.Brazelton and Morris (1996). Curr.Opin.Immunol. 8 710.
6.Magari et al (2004). Inflamm.Res. 53 544.
7.Davies, M., et al.: J. Med. Chem., 52, 2683 (2009).