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Posaconazole (trade name Noxafil) is a sterol C14α demethylase inhibitor with IC50 of 0.25 nM. Posaconazole blocks the synthesis of ergosterol by inhibiting of the enzyme lanosterol 14α-demethylase and accumulation of methylated sterol precursors. Posaconazole disrupts the close packing of acyl chains of phospholipids and impairs the functions of certain membrane-bound enzyme systems such as ATPase and enzymes of the electron transport system, thus inhibiting growth of the fungi. Posaconazole is significantly more potent at inhibiting 14-alpha demethylase than itraconazole. Oral administration of posaconazole taken with a high-fat meal exceeds 90% bioavailability and increases the concentration by four times compared to fasting state. Posaconazole is currently in a phase 2 clinical trial in Argentina testing its efficacy against asymptomatic, chronic Chagas.
| Molecular Weight | 700.78 |
| Formula | C37H42F2N8O4 |
| CAS Number | 171228-49-2 |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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