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 exhibits antifungal and antibacterial efficacy against Staphylococcus aureus, Plasmodium falciparum, Candida albicans and Candida tropicalis with MIC₅₀s of 25 μM, 0.4 μg/mL, 31 μg/mL and 62 μg/mL, respectively^[1][2].
Deacylketoconazole (0-60 μM) exhibits cytotoxicity human liver derived HepaRG cells in a dose-dependent manner with EC₅₀ of 22.8 μM^[3].

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

489.39

C₂₄H₂₆Cl₂N₄O₃

67914-61-8

ClC1=CC=C(C(Cl)=C1)[C@@]2(OC[C@H](O2)COC3=CC=C(C=C3)N4CCNCC4)CN5C=CN=C5

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]