中文名 | Merimepodib |
英文名 | Merimepodib |
别名 | 美泊地布 (S)-四氢呋喃-3-基 3-(3-(3-甲氧基-4-(恶唑-5-基)苯基)脲基)苄基氨基甲酸酯 |
英文别名 | MMP VX497 VX-497 VX 497 VI21497 VI 21497 VI-21497 VI 21497 Merimepodib MERIMEPODIB MeriMepodib, VI-21497, VX-497 (S)-Tetrahydrofuran-3-yl 3-(3-(3-methoxy-4-(oxazol-5-yl)phenyl)ureido)benzylcarbamate [(3S)-oxolan-3-yl] N-[[3-[[3-methoxy-4-(1,3-oxazol-5-yl)phenyl]carbamoylamino]phenyl]methyl]carbamate [[3-[[[[3-Methoxy-4-(5-oxazolyl)phenyl]amino]carbonyl]amino]phenyl]methyl]carbamic acid (3S)-tetrahydro-3-furanyl ester Carbamic acid, N-[[3-[[[[3-methoxy-4-(5-oxazolyl)phenyl]amino]carbonyl]amino]phenyl]methyl]-, (3S)-tetrahydro-3-furanyl ester |
CAS | 198821-22-6 |
化学式 | C23H24N4O6 |
分子量 | 452.46 |
密度 | 1.36±0.1 g/cm3(Predicted) |
沸点 | 571.4±50.0 °C(Predicted) |
溶解度 | DMSO: ≥ 31 mg/mL |
酸度系数 | 11.66±0.46(Predicted) |
存储条件 | Sealed in dry,Room Temperature |
体外研究 | VX-497 has antiproliferative effect on lymphoid and keratinocyte cells. The antiproliferative effect of VX-497 in cells is reversed within 48 h of its removal. 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 IC 50 s ranging from 6 to 19 μM. VX-497 is 100-fold more potent, with an IC 50 of 380 nM and a corresponding CC 50 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. |
体内研究 | Oral administration of VX-497 inhibits the primary IgM antibody response in a dose-dependent manner, with an ED 50 value of appr 30-35 mg/kg in mice. Single daily dosing of VX-497 is observed to be as effective as twice-daily dosing in this model of immune activation. 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.21 ml | 11.051 ml | 22.101 ml |
5 mM | 0.442 ml | 2.21 ml | 4.42 ml |
10 mM | 0.221 ml | 1.105 ml | 2.21 ml |
5 mM | 0.044 ml | 0.221 ml | 0.442 ml |
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