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编 号:F527725
分子式:C21H18N4O2
分子量:358.39
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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生物活性:
Manogepix (E1210) is a first-in-class, broad-spectrum and orally active antifungal. Manogepix has a mechanism of action-inhibition of fungal glycosylphosphatidylinositol (GPI) biosynthesis.

体内研究:
Manogepix (2.5 mg/kg, 5 mg/kg and 10 mg/kg; oral administration; twice daily; for 3 days; specific-pathogen-free female ICR mice) treatment reduces the number of viable C. albicans cells in the oral cavity in a dose-dependent manner.Animal Model:Specific-pathogen-free female ICR mice (5 weeks; ~25 g) with C. albicans
Dosage:2.5 mg/kg, 5 mg/kg and 10 mg/kg
Administration:Oral administration; twice daily; for 3 days
Result:Reduced the number of viable C. albicans cells in the oral cavity in a dose-dependent manner.

体外研究:
Manogepix inhibits the inositol acylation activity of C. albicans Gwt1p and A. fumigatus Gwt1p with IC50s of 0.3 to 0.6 μM but has no inhibitory activity against human Pig-Wp even at concentrations as high as 100 μM. To confirm the inhibition of fungal glycosylphosphatidylinositol (GPI) biosynthesis, expression of ALS1 protein, a GPI-anchored protein, on the surfaces of C. albicans cells treated with Manogepix is studied and shown to be significantly lower than that on untreated cells. Manogepix inhibits germ tube formation, adherence to polystyrene surfaces, and biofilm formation of C. albicans at concentrations above its MIC.
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