S87965 |
E1210 |
源叶(MedMol) | 98% |
- 产品描述: 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
- 靶点: Fungal;Antifungal
- 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
- 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.
- 参考文献:
1. Watanabe NA, et al. E1210, a new broad-spectrum antifungal, suppresses Candida albicans hyphal growth through inhibition of glycosylphosphatidylinositol biosynthesis. Antimicrob Agents Chemother. 2012 Feb;56(2):960-71. 2. Hata K, et al. Efficacy of oral E1210, a new broad-spectrum antifungal with a novel mechanism of action, in murine models of candidiasis, aspergillosis, and fusariosis. Antimicrob Agents Chemother. 2011 Oct;55(10):4543-51.
- 溶解性: Soluble in DMSO
- 保存条件: -20°C
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.79 ml 13.951 ml 27.903 ml 5 mM 0.558 ml 2.79 ml 5.581 ml 10 mM 0.279 ml 1.395 ml 2.79 ml 50 mM 0.056 ml 0.279 ml 0.558 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)