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VX-148

CAT: 0804-HY-118917Size: 1 EachDry Ice: NoHazardous: No
CAT#:0804-HY-118917Size:1 Each
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
CAS Number
[297730-05-3]
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

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