VX-148

• Description :

  VX-148 is an orally active immunosuppressant, which is a non-competitive inosine-5'-monophosphate dehydrogenase (IMPDH) inhibitor with Ki 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].

• UNSPSC :

  12352005

• Target :

  IMPDH

• Related Pathways :

  Metabolic Enzyme/Protease

• Applications :

  COVID-19-immunoregulation

• Field of Research :

  Inflammation/Immunology

• Smiles :

  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

• Molecular Formula :

  C23H25N5O4

• Molecular Weight :

  435.48

• References & Citations :

  [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.

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  IMPDH1; IMPDH2

• CAS Number :

  [297730-05-3]