VX-148

VX-148 is an orally active immunosuppressant, which is a non-competitive inosine-5'-monophosphate dehydrogenase (IMPDH) inhibitor with K_i values for IMPDH Ⅱ and IMPDH Ⅰ of 6 and 14 nM respectively. VX-148 can significantly inhibit the proliferation of human peripheral blood mononuclear cells (PBMC) stimulated by T-cell mitogen (PHA) or B-cell mitogen (SPAS). VX-148 has high selectivity for lymphocytes (such as L1210, Jurkat T cells, and Raji B cells), but has no significant toxicity to non-lymphoid cells. VX-148 can inhibit antibody responses in mouse models and significantly prolong the survival time of transplanted skin in allogeneic skin transplantation models. VX-148 can be used in the research of autoimmune diseases (such as rheumatoid arthritis, psoriasis) and organ transplantation anti-rejection^[1][2].