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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.
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 |
Related Cytochrome P450 (e.g. CYP17) Products |
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MS-PPOH
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(3S,5S)-Atorvastatin sodium salt is a pregnane X receptor (PXR) activator and the inactive enantiomer of Atorvastatin. |
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