Cytochrome P450 1A2 (CYP1A2) Induction Measurement Service

CYP1A Enzyme

CYP1A2 plays a significant role in metabolizing various drugs and environmental chemicals. In a CYP1A2 induction assay, cells or tissues are treated with the compound of interest, and the induction of CYP1A2 expression is then measured by assessing the activity or levels of the enzyme. The assay can help determine if the compound has the potential to induce CYP1A2-mediated drug metabolism, which can have implications for drug-drug interactions, toxicity, and pharmacokinetics.

A CYP assay is a method used to measure the activity and induction of specific cytochrome P450 enzymes in biological samples. These enzymes play a crucial role in metabolizing various drugs, chemicals, and toxins in the body. The assay can be used to assess the activity of specific CYP enzymes, such as CYP1A2, CYP2C9, CYP2D6, and others, by measuring the rate of metabolite formation from a substrate that is specific to the enzyme being tested.

Table 1 List of CYP1A2 substrates, inducers and inhibitors.

CYP1A2 Substrate CYP1A2 Inducer CYP1A2 Inhibitor
Alosetron
Amitriptyline
Caffeine
Clozapine
Duloxetine
Melatonin
Olanzapine
Pirfenidone
Ramelteon
Ramosetron
R-warfarin
Tasimelteon
Theophylline
Tizanidine
Carbamazepine
Lansoprazole
Modafinil
Omeprazole
Phenobarbital
Phenytoin
Rifampin
Ritonavir
Teriflunomide
Tobacco smoke
Acyclovir
Allopurinol
Amiodarone
Cimetidine
Enoxacin
Fluoroquinolones
Fluvoxamine
Methoxsalen
Mexiletine
Oral contraceptives
Verapamil
Zafirlukast

CYP1A2 Induction Assay Service

At Creative Biolabs, we offer a CYP1A2 induction assay service that assesses the induction potential of test compounds on CYP1A2 enzyme activity. In the assay, hepatocytes are treated with test compounds or inducers, and the mRNA levels or enzyme activity of specific CYP1A2 enzymes are measured. It isn't recommended to measure the enzyme's activity only as the induction could potentially be masked in the presence of concurrent inhibition. It would be beneficial to detect the CYP1A2 mRNA level by qPCR to enhance the analytical capabilities and accuracy of the assay. Therefore, combining the detection of mRNA levels along with enzyme activity assessment in the CYP1A2 induction assay can provide a more comprehensive analysis of CYP induction. This approach allows for a deeper understanding of the effects of various compounds on both gene expression and enzyme function.

CYP1A Induction Assay Protocol

Cell Type Human hepatocytes (1 or 3 donor(s) available)
Concentration 3-6 concentrations
The number of concentrations depends on your requirements
Replicate 3 replicates
Control A set of known positive and negative inducers
Exposure Period 72 hours
Analysis Method qRT-PCR for relative mRNA expression levels
HPLC-MS/MS quantification for enzyme activity levels
Data Delivery Full report, EC50 / Emax data

Collaborating with Creative Biolabs

Creative Biolabs provides one-stop CYP induction and CYP inhibition assays. We have a team of experts who will help you with your CYP induction assay and other ADME studies. Feel free to inquire further about this service or any other related services we offer. If you are interested in our CYP1A2 Induction Assay service, please feel free to inquire further about this service or any other related services we offer.

Support Data

Data 1: To detect the effects of omeprazole, phenobarbital, or rifampicin on CYP enzymes, the HepaMN cells were incubated with these potential inducers for 24 h. The result indicated that Zebularine induced the expression of CYP2B6.

Host cell: HepaMN cells

Candidate inducers: omeprazole, phenobarbital, and rifampicin

Detection of CYP genes: CYP1A1, CYP1A2, CYP2B6 and CYP3A4

Exposure time: 24h

Detection method: qRT-PCR

Fig.1 CYP mRNA induction after drug treatment. (Nishiwaki, et al., 2020)Fig.1 qRT-PCR analysis of CYP1A1, CYP1A2, CYP2B6, and CYP3A4 expression.1,2

References

  1. Nishiwaki, Manami, et al. "Immortalization of human hepatocytes from biliary atresia with CDK4R24C, cyclin D1, and TERT for cytochrome P450 induction testing." Scientific Reports 10.1 (2020): 17503.
  2. Distributed under Open Access license CC BY 4.0, without modification.

For Research Use Only | Not For Clinical Use

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