Merimepodib 是一种新型非竞争性肌苷一磷酸脱氢酶抑制剂，具有广谱抗病毒活性。

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

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].

Oral administration of VX-497 inhibits the primary IgM antibody response in a dose-dependent manner, with an ED50 value of appr 30-35 mg/kg in mice. Single daily dosing of VX-497 is shown to be as effective as twice-daily dosing in this model of immune activation[1]. GVHD developed in the vehicle-treated allografted F1 mice and treatment with VX-497 improved all manifestations of the disease significantly. The 2.9-fold increase in spleen weight in allografted animals is reduced to a 1.6-fold increase in the VX-497-treated mice. Serum IFN-gamma levels are increased 54-fold in the vehicle group while there is a 7.4-fold increase in VX-497-treated animals[3].

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.

198821-22-6

C23H24N4O6

452.467

美泊地布;VX-497;VI-21497

DMSO:31 mg/mL (68.51 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years