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Ketoconazole-d3 is intended for use as an internal standard for the quantification of ketoconazole by GC- or LC-MS. Ketoconazole is a broad-spectrum triazole antifungal agent that has activity against C. albicans, C. krusei, C. tropicalis, C. glabrata, C. parapsilosis, C. neoformans, and A. fumigatus strains (IC50s = 0.031-8 μg/ml). It inhibits the fungal cytochrome P450 (CYP) isoform CYP51, also known as lanosterol 14α-demethylase, which arrests ergosterol biosynthesis at the fungal membrane. Ketoconazole also inhibits human CYP3A4 (IC50 = 0.54 μM). Formulations containing ketoconazole have been used in the treatment of fungal infections.

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