| Assay Method Information | |
| | Evaluation of the Inhibition by the Compounds of Formula (I) of the Midazolam Hydroxylation by the Enzyme CYP450 3A4 |
| Description: | CYP3A4 inhibition was studied using midazolam 1′-hydroxylation as marker reaction. Midazolam was used at a single concentration of 5 NM around its Km (Michaelis-Menten constant) and the test compounds were incubated at eight different concentrations, up to 50 μM. Nicardipine was used as positive control. Microsomal incubations were initiated by the addition of NADPH-regenerating system and terminated by adding an excess of ice-cold organic solvent. The formation of 1′-hydroxymidazolam was measured by liquid chromatography-tandem mass spectrometry (LC/MS-MS) and IC50 values were calculated. |
| Affinity data for this assay | |
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