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Ketoconazole | Cytochrome P450 inhibitor

Ketoconazole (65277-42-1) is a broad spectrum antifungal agent which acts via inhibition of a cytochrome P450, CYP51A1 which is a lanosterol 14α-demethylase.1 Also inhibits CYP3A and CYP1A1.2 Inhibits adrenal steroidogenesis.3 Downregulates cholesterol synthesis in drug-tolerant human lung cancer cell lines.4 Blocks the biosynthesis of leukotrienes (LT) via inhibition of 5-lipoxygenase and dose dependently inhibits LT-mediated bronchoconstriction in guinea pigs.5

1) Lambert et al. (1986) The effects if ketoconazole on adrenal and testicular steroidogenesis in vitro; Biochem. Pharmacol. 35 3999
2) Sai et al. (2000) Assessment of specificity of eight chemical inhibitors using cDNA-expressed cytochromes P450. Xenobiotica 30 327
3) Loose et al. (1983) Ketoconazole blocks adrenal steroidogenesis by inhibiting cytochrome P450-dependent enzymes; J. Clin. Invest. 71 1495
4) Howell et al. (2019) Lung cancer cells survive epidermal growth factor receptor tyrosine kinase inhibitor exposure through upregulation of cholesterol synthesis; FASEB Bioadv. 2 90
5) Beetens et al. (1986) Ketoconazole inhibits the biosynthesis of leukotrienes in vitro and in vivo; Biochem. Pharmacol. 35 883

Focus Biomolecules cell signaling reagent supplier, structure Ketoconazole | Cytochrome P450 inhibitor | CAS 65277-42-1

Catalog#  10-1015-0100

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Catalog Number:
Cytochrome P450 inhibitor
Chemical Name:
Molecular Weight:
Molecular Formula:
Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 20 mg/ml).
Physical Properties:
Off-white solid
>98% by TLC
Storage Temperature:
Stable for 2 years as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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