Leflunomide

Appearance:

off white crystalline solid

Molecular Weight:

270.21

Density:

1.392 g/cm³

Boiling Point:

289.3 °C at 760 mmHg

Melting Point:

163-168℃

Flash Point:

128.8 °C

Storage Temperature:

2-8°C

Solubility:

Insoluble

Biological Activity:

Immunosuppressant agent. In vitro the active metabolite A77 1726 (RS-61980) inhibits dihydroorotate dehydrogenase (K i = 2.7 μ M) 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 (IC 50 = 21-27 μ g/ml). In vivo reduces inflammation in several animal models of autoimmune disease, arthritis, asthma and graft rejection.

Usage:

An immunosuppressive. 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. Therape