297730-05-3
Chemical Structure
VX-148
- No. CAS: 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 IMPDH inhibitor. VX-148 reversibly and non-competitively inhibits human IMPDH type I and type II at the NAD cofactor binding site (with Ki of 14 nM and 6 nM, respectively), blocks the de novo biosynthesis of guanine nucleotides, and selectively inhibits the proliferation of mitogen-stimulated lymphocytes. VX-148 inhibits the primary antibody response to sheep red blood cells in mice, prolongs skin graft survival in MHC-mismatched mouse models, and can be used for research on skin transplant rejection[1][2].
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VX-148 | VX-148 is an orally active IMPDH inhibitor. VX-148 reversibly and non-competitively inhibits human IMPDH type I and type II at the NAD cofactor binding site (with Ki of 14 nM and 6 nM, respectively), blocks the de novo biosynthesis of guanine nucleotides, and selectively inhibits the proliferation of mitogen-stimulated lymphocytes. VX-148 inhibits the primary antibody response to sheep red blood cells in mice, prolongs skin graft survival in MHC-mismatched mouse models, and can be used for research on skin transplant rejection. | |||||||||||||||||||||
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References
- [1]. 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 Sep;302(3):1272-7.
- [2]. Shin WJ, et al. Identification of a Small Benzamide Inhibitor of Influenza Virus Using a Cell-Based Screening. Chemotherapy. 2016;61(3):159-66.
