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编 号:F620966
分子式:C22H21N4O6P
分子量:468.4
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1mg
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5mg
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10mg
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生物活性:
Fosmanogepix (APX001) is a broad-spectrum agent against invasive fungal infections. Fosmanogepix (APX001) targets the conserved Gwt1 enzyme required for the localization of glycosylphosphatidylinositol-anchored mannoproteins in fungi. This inhibition prevents the appropriate localization of cell wall mannoproteins, which compromises cell wall integrity, biofilm formation, germ tube formation, and fungal growth. Fosmanogepix (APX001) can be used for invasive fungal infections research.

体内研究:
Fosmanogepix (APX001) (390 mg/kg, 口服给药,每天三次) 降低小鼠隐球菌性脑膜炎 (CM) 模型的真菌负荷。Fosmanogepix (APX001) (100 mg/kg, 口服给药) 在 CD-1 小鼠中是疗效的驱动因素。Animal Model:murine model of cryptococcal meningitis
Dosage:390 mg/kg
Administration:Oral gavage (p.o.)
Result:Observed significant differences (P < 0.05) fungal burden and reduced the fungal burden compared to untreated control in the lung tissue.Reduced the fungal burden of 0.78 log10 CFU/g compared with control group in brain tissue.
Animal Model:CD-1 mice
Dosage:100 mg/kg
Administration:Intraperitoneal injection (i.p.)
Result:Extended the half-life of the active moiety, APX001A, from 1.3 to 8.8 h, resulting in a 9-fold increase in the area under the curve (AUC).

体外研究:
Fosmanogepix (APX001) (2-0.002 μg/ml, 40-72小时) 抑制新生梭菌、加蒂梭菌、白色念珠菌和烟曲霉生长的最低有效浓度为 0.008-0.25 μg/ml。
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