In Vitro Cytochrome P450 3A4 (CYP3A4) Intrinsic Clearance Measurement Service
CYP3A4
CYP3A4 is an essential enzyme in the liver responsible for metabolizing a wide variety of drugs and foreign substances in the body. This enzyme is crucial for the metabolism of over half of commonly prescribed medications, such as chloroquine, acetaminophen, and diazepam. Interactions with CYP3A4 can impact the effectiveness of drugs and may lead to potential drug interactions. Understanding if certain compounds or drugs are metabolized by CYP3A4 is crucial in drug development and research. This knowledge allows researchers to predict and assess changes in drug metabolism and efficacy, aiding in the development of safe and effective medications.
CYP3A4 Intrinsic Clearance Measurement Service
At Creative Biolabs, we offer cutting-edge CYP reaction phenotyping assays using recombinant human CYPs to assess the intrinsic clearance of test compounds. Our expertise in human CYP3A4 reaction phenotyping assays allows us to offer reliable and efficient services to support pharmaceutical research and development efforts. By employing recombinant human CYP3A4, we accurately assess if test compounds are substrates metabolized by CYP3A4, a key enzyme involved in drug metabolism. The intrinsic clearance of the substrate is determined by quantifying the initial and remaining parent compounds in the reaction. This information is crucial in the drug discovery process as it can assist in predicting how a drug will be metabolized in the body, aiding in decisions regarding dosage, administration, and potential interactions with other medications.
Additionally, our laboratory offers CYP3A4 reaction phenotyping assay by utilizing liver microsomes in combination with specific chemical inhibitors. Our team is dedicated to providing high-quality data and insights that can significantly impact the success of drug development programs. Partnering with our lab for CYP phenotyping assays can help streamline the drug discovery process and enhance the overall success rate of new therapeutic agents.
CYP3A4 Phenotyping Assay Protocol
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Test System
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Recombinant human CYP3A4
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Substrate
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Test compound
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Test Concentration
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Custom concentrations available
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Test Compound Requirement
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For screening studies, 1-2 mg dry powder or 100 µL of 10 mM stock solution
For dose-response assay, 1.5-2 mg dry powder or 250 µL of 10 mM stock solution
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Replicate
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3 replicates
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Exposure Period
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15 min pre-incubation and 0, 15, 30, 60, and 90 min with NADPH at 37°C
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Negative Controls
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cDNA expressed control preparation (no CYP enzyme present)
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Analysis Method
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HPLC-MS/MS quantification
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Data Delivery
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% remaining of parent compounds at each time point
Intrinsic clearance (CLint)
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Highlights
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High specificity and sensitivity in identifying CYP3A4 metabolism of test compounds
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Comprehensive analysis of substrate depletion and metabolite formation
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Utilization of the latest techniques and recombinant human CYP3A4 enzymes
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Customized assay design to meet the specific needs of each drug discovery project
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Expert interpretation and reporting of results to aid in decision-making processes for drug development.
For Research Use Only | Not For Clinical Use
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