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Cat. No. M2058
Ketoconazole Structure


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100mg USD 60 In stock
500mg USD 160 In stock
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Biological Activity

Ketoconazole is an imidazole-containing small molecule inhibitor of cytochrome P-450. It is an inhibitor of CYP17A1, CYP3A4 and CYP3A5. Ketoconazole inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively. Ketoconazole also inhibits TXA Synthase (thromboxane synthetase) and 5-LO (5-lipoxygenase) activity. Ketoconazole induces a decrease of the number of cells in S phase and a corresponding increase of the percentage of cells in Go-G1 in HT29-S-B6 cells. Ketoconazole (25 mg/kg, i.p.) significantly decreased plasma corticosterone and reduced low dose cocaine self-administration without affecting food-reinforced responding. Ketoconazole is currently in a phase 2 clinical trial with Prostate Cancer.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 531.43
Formula C26H28Cl2N4O4
CAS Number 65277-42-1
Purity 99.91%
Solubility DMSO 20 mg/mL
Ethanol 10 mg/mL
Storage at -20°C

Ketoconazole reduces low dose cocaine self-administration in rats.
Goeders NE, et al. Drug Alcohol Depend. 1998 Dec 1;53(1):67-77. PMID: 10933341.

In vitro susceptibility of the seven Malassezia species to ketoconazole, voriconazole, itraconazole and terbinafine.
Gupta AK, et al. Br J Dermatol. 2000 Apr;142(4):758-65. PMID: 10792228.

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Abmole Inhibitor Catalog 2017

Keywords: Ketoconazole, (±)-Ketoconazol supplier, CYP17, inhibitors

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