Ketoconazole | Cytochrome P450 Inhibitor

CAS:
65277-42-1
Catalog Number:
10-1015
Activity:
Cytochrome P450 inhibitor
Chemical Name:
(±)-1-[4-(4-{[-2-(2,4-Dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazin-1-yl]ethan-1-one
Molecular Weight:
531.43
Molecular Formula:
C26H28Cl2N4O4
Solubility:
Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 20 mg/ml).
Physical Properties:
Off-white solid
Purity:
>98% by TLC
Storage Temperature:
RT
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
100 mg$45.00
500 mg$75.00

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

References/Citations:

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

CAS:
65277-42-1
Catalog Number:
10-1015
Activity:
Cytochrome P450 inhibitor
Chemical Name:
(±)-1-[4-(4-{[-2-(2,4-Dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazin-1-yl]ethan-1-one
Molecular Weight:
531.43
Molecular Formula:
C26H28Cl2N4O4
Solubility:
Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 20 mg/ml).
Physical Properties:
Off-white solid
Purity:
>98% by TLC
Storage Temperature:
RT
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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