ExpressPlus CYP IC50 in Human Liver Microsomes Using LC-MS/MS

This assay is used to determine the IC50 for reversible inhibition of individual cytochrome P450 (CYP) enzymes by a test compound.

Catalog number EA427

Required from Customer

Deliverables

Substrate

Assay System

Assay Conditions

Assay QC

Notes

  1. The results from this assay are sent to the customer in the ExpressPlus report format, which may include graphical representations of data and comparison with historical data for reference compounds.
  2. IC50 values are estimated by fitting the experimental data (percent of control activity remaining at each concentration of test compound) to a sigmoidal model and non-linear regression analysis.
Individual CYP Substrates and Positive Control Inhibitors 
CYP Isoform Probe Substrate Metabolite Positive Control Inhibitor
1A2 Phenacetin Acetaminophen α-Naphthoflavone
2A6 Coumarin 7-OH coumarin Tranylcypromine
2B6 Bupropion Bupropion Thio-TEPA
2C8 Amodiaquine Desethylamodiaquine Montelukast
2C9 Diclofenac 4’-OH diclofenac Sulfaphenazole
2C19 S-mephenytoin 4’-OH mephenytoin (+)-N-3-benzylnirvanol
2D6 Bufuralol 1’-OH bufuralol Quinidine
2E1 Chlorzoxazone 6-OH chlorzoxazone 4-Methylpyrazole
3A4 Testosterone 6β-OH testosterone Ketoconazole
Midazolam 1’-OH midazolam