Cytochrome P450 2C8 (CYP2C8) Induction Measurement Service

CYP2C8

Cytochrome P450 2C8 (CYP2C8) is a member of the cytochrome P450 enzyme family, involved in the metabolism of various endogenous and exogenous substances. It is mainly expressed in the liver but has also been found in other tissues like the intestine, kidneys, and brain. CYP2C8 is involved in the metabolism of various drugs, including antidiabetic medications like rosiglitazone and repaglinide, as well as chemotherapeutic agents like paclitaxel. In addition to its role in drug metabolism, CYP2C8 is also known for its epoxygenase activity, catalyzing the oxidation of arachidonic acid to epoxyeicosatrienoic acids (EETs), which are potent signaling molecules involved in regulating vascular tone, inflammation, and other physiological processes.

Table 1. Some CYP2C8 substrates, inducers and inhibitors.

CYP2C8 Substrate CYP2C8 Inducer CYP2C8 Inhibitor
Amodiaquine
Cerivastatin
Montelukast
Paclitaxel
Pioglitazone
Repaglinide
Rosiglitazone
Torsemide 		Hyperforin
Phenobarbital
Rifampin 		Clopidogrel
Deferasirox
Gemfibrozil
Ketoconazole
Montelukast
Telithromycin
Teriflunomide
Trimethoprim

CYP2C8 Induction Assay Service

Creative Biolabs is dedicated to providing in vitro ADME service for comprehensive and reliable assessment of the pharmacokinetic properties of test compounds.

With cutting-edge technology and expert scientific support, we offer a CYP2C8 induction assay that assesses the potential of a compound to induce the activity of the CYP2C8 enzyme. The assay involves the use of human hepatocytes, incubated with test compounds, to measure the induction of the CYP2C8 enzyme. Appropriate positive and negative controls are included in our assay, such as untreated cells or cells treated with a known CYP2C8 inducer, for comparison. We carry out qRT-PCR to evaluate the relative expression levels of CYP2C8 in response to the treatment. We also assess CYP2C8 enzyme activity by analyzing metabolites produced during the metabolism of specific substrates. This comprehensive approach provides valuable insights into the potential induction of CYP2C8 and its impact on drug metabolism and interactions.

CYP2C8 Induction Assay Protocol

Cell Type Hepatocytes
Test Article Concentration The number of concentrations varies based on your specific needs.
Replicate 3 replicates
Substrates for Catalytic Activity Amodiaquine
Control Positive control and negative control
Incubation 72 hours (media changed every 24 hours)
Analysis Method Two methods are available:
  • qRT-PCR for CYP2C8 mRNA expression levels
  • Enzyme activity: quantification of N-desethylamodiaquine by HPLC-MS/MS
Data Delivery Full report, raw data. The EC50 and Emax will be provided if applicable.

Our in vitro ADME services offer a comprehensive platform for evaluating the pharmacokinetic properties of compounds and assessing their potential for drug-drug interactions. Please contact us to support your drug discovery and development efforts.

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