E1210

936339-60-5

358.39

DMSO : 100 mg/mL (279.03 mM; Need ultrasonic)

Anti-infection

E1210 is a first-in-class, broad-spectrum and orally active antifungal. E1210 has a mechanism of action-inhibition of fungal glycosylphosphatidylinositol (GPI) biosynthesis^[1][2]. IC50 & Target: Fungal^[1][2] In Vitro: E1210 inhibits the inositol acylation activity of C. albicans Gwt1p and A. fumigatus Gwt1p with IC₅₀s of 0.3 to 0.6 uM but has no inhibitory activity against human Pig-Wp even at concentrations as high as 100 uM. 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 E1210 is studied and shown to be significantly lower than that on untreated cells. E1210 inhibits germ tube formation, adherence to polystyrene surfaces, and biofilm formation of C. albicans at concentrations above its MIC^[1]. In Vivo: E1210 (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^[2].