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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 |
|---|
| Abiraterone
Abiraterone acetate (CB-7598) is a potent, selective, and orally available inhibitor of CYP17 with an IC50 of 4 nM. |
| Avasimibe
Avasimibe (CI-1011) is a novel orally bioavailable ACAT inhibitor with IC50 values of 2.9, 13.9, 26.5 µM for CYP2C9, CYP1A2 and CYP2C19, respectively. |
| Imidaclopride
Imidaclopride is a systemic insecticide which acts as an insect neurotoxin and belongs to a class of chemicals called the neonicotinoids. |
| Chrysin
Chrysin is a naturally occurring flavone chemically extracted from the passion flowers Passiflora caerulea. |
| Chlorzoxazone
Chlorzoxazone is a probe for human liver cytochrome P-450IIE1. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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