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Ketoconazole

Cat. No. M2058
Ketoconazole Structure
Synonym:

(±)-Ketoconazol

Size Price Availability Quantity
100mg USD 50  USD50 In stock
500mg USD 75  USD75 In stock
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Quality Control
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 531.43
Formula C26H28Cl2N4O4
CAS Number 65277-42-1
Purity 99.91%
Solubility DMSO 3 mg/mL
Ethanol 7 mg/mL
Storage at -20°C
References

[1] Goeders NE, et al. Drug Alcohol Depend. Ketoconazole reduces low dose cocaine self-administration in rats.

[2] Gupta AK, et al. Br J Dermatol. In vitro susceptibility of the seven Malassezia species to ketoconazole, voriconazole, itraconazole and terbinafine.

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Keywords: Ketoconazole, (±)-Ketoconazol supplier, Cytochrome P450 (e.g. CYP17), inhibitors

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