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), with IC₅₀ values of 82 nM and 73 nM respectively. VX-148 has high selectivity for lymphocytes (such as L1210, Jurkat T cells, and Raji B cells), with IC₅₀ values ranging from 245 to 511 nM, 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].

435.48

C₂₃H₂₅N₅O₄

297730-05-3

O=C(O[C@@H](CC#N)CC)N[C@H](C1=CC=CC(NC(NC2=CC=C(C#N)C(OC)=C2)=O)=C1)C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Pankiewicz KW,et al. Cofactor mimics as selective inhibitors of NAD-dependent inosine monophospate dehydrogenase (IMPDH)-the major therapeutic target. Current medicinal chemistry. 2004 Apr 1;11(7):887-900.

  [2]. Jain J, et al. Characterization of pharmacological efficacy of VX-148, a new, potent immunosuppressive inosine 5′-monophosphate dehydrogenase inhibitor. The Journal of pharmacology and experimental therapeutics. 2002 Jan 1;302(3):1272-7.