In Vitro Cytochrome P450 2C8 (CYP2C8) Intrinsic Clearance Measurement Service
Cytochrome P450 (CYP) reaction phenotyping studies are used to determine which specific CYP enzymes are responsible for metabolizing a particular drug or compound in the body. By conducting these studies, researchers can better understand how different CYP enzymes contribute to drug metabolism and drug-drug interactions, which can help in the development of safer and more effective medications. Creative Biolabs offers comprehensive CYP phenotyping assays for evaluating a wide range of CYP isoforms, including 2C8, 2C9, and 2B8. These assays are designed to assess the metabolic activities of specific CYP isoforms to understand their role in drug metabolism and potential drug-drug interactions.
CYP2C8 Phenotyping Assay
The CYP2C8 phenotyping assay is a type of in vitro experiment used to evaluate the role of the CYP2C8 enzyme in drug metabolism, predict potential drug-drug interactions, study metabolic stability, and optimize drug dosing strategies. At Creative Biolabs, our comprehensive services include designing, executing, and analyzing CYP2C8 reaction phenotyping studies to support your research and drug development needs. By using recombinant human CYP2C8 enzymes, we can evaluate the enzyme's ability to metabolize specific substrates, providing valuable insights into drug interactions, efficacy, and safety. This assay involves incubating the enzyme with a known substrate and measuring the rate of metabolism to determine the enzyme's intrinsic clearance or activity. Various analytical techniques such as LC-MS are used to quantify the parent compound in the reaction mixture.
Sample Submission
A dry compound (~1 to 2 mg) or 100 μL of 10 mM stock solution is required for the screen studies.
For dose-response assays, dry compound (~1.5 to 2 mg) or 250 μl of 10 mM stock solution may be sufficient.
Assay System
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Individually expressed recombinant human CYP2C8
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The test compound is incubated with CYP2C8 in the presence of NADPH.
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The remaining parent compound at each time point is measured by HPLC-MS/MS.
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The metabolic intrinsic clearance (CLint) is determined by measuring linear depletion rates of the parent drugs in the presence of recombinant CYP2C8.
Data Delivery
Data include parent compound percent remaining, half-life, and clearance values. The full study report is provided.
Working with Creative Biolabs
Creative Biolabs is dedicated to offering a comprehensive suite of phenotyping assays to support your in vitro ADME research. A wide range of CYP intrinsic clearance measurements at our lab are used to assess the capacity of an enzyme system to metabolize a drug substance and are often utilized in metabolic stability studies to predict the in vivo clearance of a compound. Contact us now to learn more about our CYP phenotyping services and how we can support your research and development efforts.
For Research Use Only | Not For Clinical Use
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