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Ketoconazole

Cat. No. M2058
Ketoconazole Structure
Synonym:

(±)-Ketoconazol; KTZ

Size Price Availability Quantity
100mg USD 50  USD50 In stock
500mg USD 75  USD75 In stock
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Quality Control & Documentation
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.

Chemical Information
Molecular Weight 531.43
Formula C26H28Cl2N4O4
CAS Number 65277-42-1
Solubility (25°C) DMSO 3 mg/mL
Ethanol 7 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

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; KTZ supplier, Cytochrome P450 (e.g. CYP17), inhibitors, activators


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