CYP Inhibition



Overview

Sekisui XenoTech's Discovery Plus™ Inhibition is more than just a screening service. Our 96-well plate format offers data for the seven enzymes recommended by regulatory agencies for both direct and time-dependent inhibition. Discovery Plus™ Inhibition is a non-GLP service that quickly provides customers with a data summary of results. This service is best utilized for compounds that are in the early discovery phase/early development phase. For compounds that will be submitted for regulatory agency approval, please visit our standard CYP inhibition service page.

View Sekisui XenoTech's Discovery Plus™ Inhibition Poster
 

IC50 Determinations

Sekisui XenoTech offers the ability to perform IC50 experiments based on values that are calculated from area ratios with the flexibility to evaluate direct inhibition and time-dependent inhibition using a seven substrate cocktail. The global P450 inhibitor, 1-aminobenzotriazole (1-ABT), can be added as a positive control upon request.

Cocktail Substrate:
 
Enzyme Substrate
CYP1A2 Phenacetin O-dealkylation
CYP2B6 Bupropion hydroxylation
CYP2C8 Paclitaxel 6α-hydroxylation
CYP2C9 Diclofenac 4´ -hydroxylation
CYP2C19 S-Mephenytoin 4´ -hydroxylation
CYP2D6 Dextromethorphan O-demethylation
CYP3A4/5 Midazolam 1´ -hydroxylation
 

Test System & Incubation Conditions

Test system: pool of 16 individuals, mixed gender, human liver microsomes
Designed to minimize inhibitor and substrate depletion
Zero-minute (direct) and/or 30-minute (time-dependent) pre-incubation
Robotic incubations
 

Results

A tabulated summary of IC50 values will be provided
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Enzyme Induction
Drug Transporter Inhibition
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