Mycophenolate Mofetil (TM-MMF), an immunosuppressive agent, is the 2-morpholinoethyl ester of mycophenolic acid (MPA), and an inhibitor of inosine monophosphate dehydrogenase (IMPDH).

IMPD type I:39 nM, IMPD type II:27 nM

As an ester prodrug of the active immunosuppressant mycophenolic acid, Mycophenolate mofetil (10 μg/mL) significantly induces apoptosis in microglial cell cultures and increases the number of apoptotic cells due to activated caspase-3 immunoreactivity. At a concentration of 1 μg/mL, Mycophenolate mofetil also potently inhibits the proliferation of astrocytes and microglia. Recent studies have shown that following neuronal injury, Mycophenolate mofetil significantly reduces the extent of neuronal cell death in organotypic hippocampal slice cultures in a time-dependent manner. Mycophenolic acid inhibits the activity of both type I/II isocitrate dehydrogenase in a non-competitive, reversible, and selective manner, with IC50 values of 39 nM and 27 nM, respectively. Moreover, it concentration-dependently inhibits the proliferation of ConA-stimulated T cells (IC50 = 100 nM), lipopolysaccharide-stimulated B cells (IC50 = 120 nM), and alloantigen-specific T cell proliferation (IC50 = 51 nM).

At a high concentration of 10 μg/mL, Mycophenolate mofetil induces significant apoptosis in microglial cell cultures and increases the number of apoptotic cells exhibiting elevated levels of activated caspase-3 immunoreactivity. Furthermore, at 1 μg/mL, it strongly inhibits the proliferation of microglia and astrocytes. Recent studies have demonstrated that Mycophenolate mofetil significantly attenuates the extent of neuronal death in organotypic hippocampal slice cultures following neuronal injury in a time-dependent manner. Mycophenolate mofetil, an active immunosuppressive ester prodrug of mycophenolic acid, exhibits non-competitive, selective, and reversible inhibition of inosine monophosphate dehydrogenase type I/II, with IC50 values of 39 nM and 27 nM, respectively. Moreover, mycophenolic acid, the immunosuppressive agent, also inhibits the proliferation of T cells stimulated by ConA, B cells stimulated by lipopolysaccharide, and allospecific T cells in a concentration-dependent manner, with IC50 of 100 nM, 120 nM, and 51 nM, respectively.