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Merimepodib

Catalog No. T3444   CAS 198821-22-6
Synonyms: VX-497, VI-21497

Merimepodib (VX-497) is a novel noncompetitive inhibitor of Inosine monophosphate dehydrogenase(IMPDH).

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Merimepodib Chemical Structure
Merimepodib, CAS 198821-22-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 39.00
5 mg In stock $ 91.00
10 mg In stock $ 163.00
25 mg In stock $ 297.00
50 mg In stock $ 538.00
100 mg In stock $ 777.00
1 mL * 10 mM (in DMSO) In stock $ 90.00
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Purity: 99.31%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Merimepodib (VX-497) is a novel noncompetitive inhibitor of Inosine monophosphate dehydrogenase(IMPDH).
In vitro VX-497 has antiproliferative effect on lymphoid and keratinocyte cells. VX-497 (MW 452.5) is orally bioavailable and inhibits the proliferation of primary human, mouse, rat, and dog lymphocytes at concentrations of approximately 100 nM. The antiproliferative effect of VX-497 in cells is reversed within 48 h of its removal[1]. VX-497 has intermediate antiviral activity against a second group of viruses, which includes HSV-1, parainfluenza-3 virus, BVDV, VEEV, and dengue virus, with IC50s ranging from 6 to 19 μM. VX-497 is 100-fold more potent, with an IC50 of 380 nM and a corresponding CC50 of 5.2 μM, for a therapeutic index of 14. The antiviral activity of VX-497 in HepG2.2.2.15 cells is reversed threefold by the addition of guanosine[2].
In vivo Administering VX-497 orally attenuates the primary IgM antibody response in mice in a dose-dependent manner, achieving an effective dose 50 (ED50) between 30-35 mg/kg. Both single and twice-daily dosing of VX-497 are comparably effective in reducing immune activation in this model[1]. In models of graft-versus-host disease (GVHD) involving allografted F1 mice, the untreated group displayed disease development, whereas VX-497 treatment significantly ameliorated disease symptoms. Specifically, VX-497 treatment decreased the spleen weight increase from 2.9-fold in untreated allografted mice to 1.6-fold, and reduced serum interferon-gamma (IFN-gamma) levels from a 54-fold increase in the control group to a 7.4-fold increase in treated mice[3].
Cell Research The murine fibroblast L929 cell line is cultured in Eagle minimal essential medium supplemented with 10% fetal bovine serum, nonessential amino acids, 50 U of penicillin per mL, 50 μg of streptomycin per mL, and 2 mM?l-glutamine. EMCV is infected at 500 PFU/107?L929 cells. Cells are left untreated or are treated with different concentrations of murine IFN-α alone, VX-497 alone, or combinations thereof.
Synonyms VX-497, VI-21497
Molecular Weight 452.46
Formula C23H24N4O6
CAS No. 198821-22-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 31 mg/mL (68.51 mM)

TargetMolReferences and Literature

1. Jain J, et al. VX-497: a novel, selective IMPDH inhibitor and immunosuppressive agent. J Pharm Sci. 2001 May;90(5):625-37. 2. Markland W, et al. Broad-spectrum antiviral activity of the IMP dehydrogenase inhibitor VX-497: a comparison with ribavirin and demonstration of antiviral additivity with alpha interferon. Antimicrob Agents Chemother. 2000 Apr;44(4):859-66. 3. Decker CJ, et al. The novel IMPDH inhibitor VX-497 prolongs skin graft survival and improves graft versus host disease in mice. Drugs Exp Clin Res. 2001;27(3):89-95.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Metabolism Compound Library Anti-Infection Compound Library Anti-Metabolism Disease Compound Library ReFRAME Related Library Bioactive Compounds Library Max Covalent Inhibitor Library Clinical Compound Library Metabolism Compound Library

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Keywords

Merimepodib 198821-22-6 Immunology/Inflammation Metabolism Microbiology/Virology Proteases/Proteasome Dehydrogenase HCV Protease Antiviral HBV HCV Inhibitor Hepatitis C virus Hepatitis B virus VX497 VX 497 inhibit MMPD VI 21497 VX-497 VI-21497 VI21497 inhibitor

 

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