The cytochrome P450 (CYP) enzyme system plays a crucial role in the metabolism of various drugs within the human body. Among these enzymes, CYP2C8 is noteworthy due to its involvement in metabolizing significant drugs, including those used in chemotherapy and diabetes treatment. Identifying inhibitory interactions with CYP2C8 is thus imperative for predicting potential drug-drug interactions (DDIs) and ensuring drug safety and efficacy. Creative Biolabs proudly offers a sophisticated CYP2C8 inhibition IC50 assessment service designed to accurately determine inhibitory constants and predict possible DDIs, thereby optimizing drug development processes.

Our CYP2C8 Inhibition IC50 Assessment Service

Inhibition of CYP2C8 can lead to substantial alterations in drug pharmacokinetics, potentially resulting in adverse drug interactions. Our specialized service at Creative Biolabs aims to evaluate this inhibition under stringent experimental conditions, providing reliable IC50 values essential for drug safety evaluations. We employ state-of-the-art techniques such as liquid chromatography-tandem mass spectrometry (LC/MS/MS) to ensure high accuracy and reproducibility.

Services Details

IC50 Determination

Our primary service involves the determination of IC50 values for various compounds to assess their inhibitory potential on CYP2C8 activity. We utilize well-characterized index reactions, such as amodiaquine-N-demethylation, in human liver microsomes (HLM) to achieve this.

Time-Dependent Inhibition Assessment

For a comprehensive understanding, we offer time-dependent inhibition (TDI) evaluations, where compounds are pre-incubated with NADPH before initiating the enzyme reaction. This method helps identifying the formation of inhibitory metabolites over time.

Our Advantage

• High-Throughput Capabilities

Our laboratories are equipped to handle high-throughput screenings, essential for large-scale drug development projects. Using liver microsomes and recombinant CYP enzymes, we ensure diverse and scalable assessments.

• Advanced Analytical Techniques

The integration of LC/MS/MS in our workflow guarantees highly sensitive and specific detection of enzymatic activities and metabolite concentrations, ensuring reliable data output.

• Expertise and Experience

With over 20 years of industry experience, Creative Biolabs stands out for its in-depth knowledge and technical prowess. Our expert team employs cutting-edge platforms and rigorous protocols to deliver unparalleled service quality.

Frequently Asked Questions

Q1: How does Creative Biolabs measure CYP2C8 inhibition?

A1: Our laboratories use an IC50 determination approach involving human liver microsomes and a specific index reaction. We employ LC/MS/MS to accurately measure inhibitory effects on CYP2C8 activity.

Q2: What additional services do you offer related to CYP inhibition?

A2: In addition to CYP2C8, we offer comprehensive inhibition assays for multiple CYP isozymes, including CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, and CYP3A. We provide both direct and time-dependent inhibition assessments.

Creative Biolabs remains committed to excellence in enzymology and DDI prediction, driving advancements in drug safety and efficacy through our state-of-the-art CYP2C8 inhibition IC50 assessment service.

For Research Use Only | Not For Clinical Use