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