In Vitro Cytochrome P450 2D6 (CYP2D6) Intrinsic Clearance Measurement Service
CYP2D6
Cytochrome P450 2D6 (CYP2D6) is a vital enzyme that is responsible for the metabolism of a wide variety of drugs in the body. Primarily found in the liver, CYP2D6 plays a key role in metabolizing many medications. In addition to its high expression in the liver, CYP2D6 is also found in the central nervous system, where it contributes to the metabolism of neurotransmitters and other endogenous compounds. CYP2D6 is associated with the metabolism of approximately one-quarter of all clinically used drugs, including antidepressants, antipsychotics, beta-blockers, and opioids. Genetic variations in the CYP2D6 gene can lead to differences in enzyme activity among individuals, resulting in variability in drug metabolism and potentially influencing drug response and toxicity.
CYP2D6 Phenotyping Assay Using Recombinant Human CYP2D6 Enzymes
At Creative Biolabs, our portfolio of in vitro ADME services includes the reaction phenotyping assay. One common method we employ for CYP2D6 phenotyping assays involves the use of recombinant CYP2D6 enzyme. Recombinant CYP2C9 enzyme can be expressed and isolated for in vitro studies to evaluate its activity towards the test drug substrate. This allows for a controlled environment to determine the enzyme kinetics and metabolic pathways involved. Our experienced team utilizes advanced technologies to accurately measure CYP2D6 intrinsic clearance rates. This assay provides clients with valuable information about how efficiently the CYP2D6 enzyme metabolizes specific drugs.
Assay Procedure
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The recombinant CYP2D6 enzyme is incubated with a test compound in the presence of a cofactor such as NADPH, which is necessary for the enzymatic activity of CYP2D6.
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The reaction mixture is incubated at a specific temperature and pH for a predetermined amount of time.
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At the end of the incubation period, the reaction is stopped and the parent compound is quantified using analytical techniques such as HPLC or LC-MS.
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The rate of metabolism, or intrinsic clearance, of the test compound by CYP2D6 is calculated based on the depletion of the parent compound over time.
Applications of CYP2D6 Phenotyping Assay
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Drug development: The assay can be used in drug development to assess the metabolism of new compounds by CYP2D6 and predict their pharmacokinetic properties in vivo.
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Pharmacokinetic modeling: Intrinsic clearance data can be incorporated into pharmacokinetic models to predict drug exposure and optimize dosing regimens, particularly for drugs with complex metabolism involving CYP2D6.
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Personalized medicine: Understanding the activity of CYP2D6 in metabolizing drugs can help healthcare providers tailor drug therapy to individual patients based on their CYP2D6 genotype.
Contact us today to learn more about our CYP2D6 intrinsic clearance measurement service and how it can benefit your research.
For Research Use Only | Not For Clinical Use
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