297730-05-3
Chemical Structure
VX-148
- CAS No.: 297730-05-3
- Formula:C23H25N5O4
- Molecular Weight:435.48
IUPAC Name: (R)-1-cyanobutan-2-yl ((S)-1-(3-(3-(4-cyano-3-methoxyphenyl)ureido)phenyl)ethyl)carbamate
InChIKey: PJFQWSNOXLEDDZ-MGPUTAFESA-N
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
Biological Activity: 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].
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VX-148 | 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. | |||||||||||||||||||||
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- [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.
Keywords
