|Cyprotex also offers cytochrome P450 induction using human hepatocytes to meet with regulatory recommendations.|
Because reporter assays are relatively high throughput and cost effective, they can be a valuable tool in drug discovery.
1Chu V, Einolf HJ, Evers R, Kumar G, Moore D, Ripp S, Silva J, Sinha V, Sinz M, and Skerjanec A (2009) Drug Metab Dispos 37; 1339-1354.
|Method||Luciferase reporter gene assay|
|Cell Lines||DPX2™ for PXR and 1A2-DRE™ cells for AhR (supplied by Puracyp)|
|Test Article Concentrations||0.1, 0.4, 1, 4, 10, 40, 100 µM (different concentrations available)|
|Quality Controls||Vehicle control
Positive control (rifampicin for PXR and omeprazole for AhR)
|Number of Replicates||2 replicates per concentration|
|Test Article Requirements||50 µL of a 100 mM DMSO solution|
|Data Delivery||Fold activation relative to vehicle control
EC50 and Emax (if appropriate)
% Cell loss at each concentration and EC50 (if appropriate)
Known activators of PXR and AhR were selected and screened in the PXR and AhR nuclear receptor activation assay. Data generated were compared to those published in the literature.
|Compound||Cyprotex EC50 (µM)||Cyprotex Emax|
|Rifampicin||1.1||25.7 at 10 µM||30.6 at 10 µM|
|Dexamethasone||24.2||9.9 at 100 µM||7.1 at 250 µM|
|Troglitazone||3.7||9.4 at 20 µM||8.3 at 50 µM|
|Omeprazole||22.4||12.5 at 100 µM||25.9 at 100 µM|
|Phenobarbital||323||19.3 at 1000 µM||13.5 at 1000 µM|
|Mifepristone||0.8||17.5 at 10 µM||9.3 at 10 µM|
1 Chu V et al., (2009) Drug Metab Dispos 37; 1339-1354
2 Yueh M-F et al., (2005) Drug Metab Dispos 33; 38-48