In Vitro Cytochrome P450 1A2 (CYP1A2) Intrinsic Clearance Measurement Service
CYP enzymes play a vital role in the metabolism of many drugs, determining their efficacy, toxicity, and pharmacokinetics. As experts in ADME, we specialize in offering CYP1A2 reaction assays to evaluate the metabolic properties of your test compounds. Our comprehensive services provide valuable insights into the intrinsic clearance and metabolism of your test compound, aiding in the drug development process.
CYP1A2 Intrinsic Clearance Measurement
The measurement of CYP1A2 intrinsic clearance involves determining the rate at which a substrate metabolizes in the presence of the enzyme. Creative Biolabs offers CYP1A2 intrinsic clearance measurement to measure the rate of metabolism or clearance of your compounds. This assay is used to evaluate the activity of CYP1A2 and can provide valuable information on drug metabolism and potential drug interactions. CYP1A2 intrinsic clearance can be measured using either recombinant CYP1A2 enzyme or human liver microsomes in a controlled environment. The remaining parent compound is assessed by HPLC-MS/MS. This data can be used to determine the kinetics of the CYP1A2-mediated metabolism and calculate parameters such as intrinsic clearance, Km, and Vmax.
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Recombinant CYP1A2 Enzyme
The test compound is incubated with recombinant CYP2C9 enzyme in the presence of NADPH. This method can assess the direct effect of the CYP2C9 enzyme individually on test compound breakdown. However, one limitation of recombinant enzymes is that they may not fully replicate the complex environment of the liver, which can affect the accuracy of the measurement.
Inhibition of CYP1A2 enzyme activity in human liver microsomes can be used to determine the intrinsic clearance of CYP1A2 substrates. By measuring the metabolism of a test compound in the presence and absence of a chemical inhibitor of CYP1A2, the contribution of CYP1A2 to the overall clearance of a test compound can be determined. Using human liver microsomes to measure intrinsic clearance provides a more physiologically relevant system that closely mimics the conditions in the human body.
Our Capabilities
The CYP phenotyping assays are designed to assess the metabolic activities of specific CYP isoforms to understand their role in drug metabolism and potential drug-drug interactions. Our services offer comprehensive and tailored solutions to assess how these CYP isoforms metabolize various test compounds to provide valuable insights into drug metabolism and potential interactions. Our team of expert scientists utilizes state-of-the-art technologies and methodologies to provide accurate and reliable results for our clients. Contact us to learn more about our CYP phenotyping services and how we can support your research and development efforts.
Support Data
Data 1: The experiment aims to determine specific CYP isoforms for the metabolism of MH. The result showed MH was mainly metabolized by CYP1A2 and CYP2C19.
Fig.1 Metabolic clearance rate of MH under CYP1A2 or CYP2C19 inhibitor.1,2
References
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Huang, Xi, et al. "Searching the cytochrome p450 enzymes for the metabolism of meranzin hydrate: a prospective antidepressant originating from Chaihu-Shugan-San." PloS one 9.11 (2014): e113819.
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Distributed under Open Access license CC BY 4.0, without modification.
For Research Use Only | Not For Clinical Use
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