CYP2C8 Inhibition Assay Service

CYP2C8 for compound screening and profiling assay using luminescence-based method to measure cytochrome P450 enzyme activity.

Target Overview
CAT#

CYP2C8

Enzyme

Human CYP2C8 + P450 Reductase microsomes

Synonym

CYP2C8; cytochrome P450 family 2, subfamily C, polypeptide 8; S-mephenytoin 4-hydroxylase

Scientific Information

P10632 (https://www.uniprot.org/uniprotkb/P10632/entry)

Assay Properties
Substrate

P450-Glo™ proluciferin Substrate

Reaction

RH + O₂ + NADPH + H⁺ = ROH + H₂O + oxidized [NADPH—hemoprotein reductase]

Readout

Enzymatic activity

Reference Compound IC50s
Compound IC50 (nM)
Ketoconazole 1300
Montelukast 55.3
Tranylcypromine >10000
Cimetidine >10000
Imipramine >10000
Verapamil >10000
Screening Location

Malvern, PA, USA

Further Information

More information can be found on our website CYP450 Inhibition Assay Services.

Reference compound IC50 for CYP2C8