Deacylketoconazole  (Synonyms: N-Deacetylketoconazole; R-39519)

Deacylketoconazole (N-Deacetylketoconazole; R-39519) is an orally active metabolite of Ketoconazole (HY-B0105). Deacylketoconazole exhibits antifungal and antibacterial activity. Deacylketoconazole is cytotoxic in rats hepatocyte^[1][2][3].

Deacylketoconazole 对 Staphylococcus aureus，Plasmodium falciparum，Candida albicans 和 Candida tropicalis 具有抗真菌和抗菌活性，MIC₅₀ 分别为 25 μM，0.4 μg/mL，31 μg/mL 和 62 μg/mL^[1][2]。
Deacylketoconazole (0-60 μM) 对人肝来源的 HepaRG 细胞具有剂量依赖性的细胞毒性，EC₅₀ 为 22.8 μM^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

489.39

C₂₄H₂₆Cl₂N₄O₃

67914-61-8

脱酰基酮康唑

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Pfaller MA, et al., Activity of ketoconazole and its deacyl derivative against Plasmodium falciparum and Candida isolates. Antimicrob Agents Chemother. 1982 Nov;22(5):917-9.  [Content Brief]

  [2]. Bossche H V, et al., Molecular basis for the antimycotic and antibacterial activity of N‐substituted imidazoles and triazoles: The inhibition of isoprenoid biosynthesis[J]. Pesticide science, 1984, 15(2): 188-198.

  [3]. Fukami T, et al., Human arylacetamide deacetylase hydrolyzes ketoconazole to trigger hepatocellular toxicity. Biochem Pharmacol. 2016 Sep 15;116:153-61.  [Content Brief]