High-throughput ADME Screening
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In the past decade to fifteen years, in vitro absorption, distribution, metabolism, and excretion (ADME) data have been pivotal in drug development. The advent of high throughput screening (HTS) has enabled the rapid and efficient evaluation of ADME properties in the early phases of drug discovery, greatly improving development efficiency by eliminating unsuitable candidates early on. Using liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS), with its high sensitivity and specificity, provides scientists with a powerful tool for more precisely studying in vitro drug behavior and predicting in vivo pharmacokinetics.
HTS technology relies on experimental methods at both the molecular and cellular levels, using microplates as experimental tools. It integrates automated systems and high-sensitivity devices to swiftly conduct experiments and collect data. Supported by databases, HTS can simultaneously test and analyze thousands of samples. Compared to traditional screening methods, HTS offers advantages such as reduced reaction volumes, high automation, rapid processing, and increased specificity. These benefits enable researchers to more efficiently identify and understand drug action mechanisms. Furthermore, these advantages significantly enhance the efficiency of drug screening and reduce the high attrition rate in drug development due to poor pharmacokinetics.
Creative Bioarray's "High-throughput ADME Screening" service employs cutting-edge HTS technology to accelerate drug development, offering clients comprehensive and precise pharmacokinetic data. By integrating automated, intelligent experimental platforms with advanced bioinformatics analysis tools, we provide robust data support to aid in the discovery and optimization of new drugs.
Brief Workflow
- Plate administration of test compounds: We test compounds in a high-density plate format, ensuring correct labeling and strict tracking for each test compound throughout the screening process to enhance efficiency and reproducibility.
- MS/MS method optimization: Optimize MS/MS methods based on the compound's characteristics, including ionization mode, collision energy, and chromatography conditions, to ensure accurate and rapid compound detection and analysis.
- In vitro ADME experiments and sample clean-up: Simulate absorption, distribution, metabolism, and excretion processes using in vitro systems to assess compound ADME properties, including cell culture experiments, enzyme reaction system experiments, and protein crystallization experiments, etc. Purify samples post-experiment to eliminate interference, enhancing analysis accuracy and sensitivity.
- Raw LC-MS/MS data collection and analysis: Collect raw data using LC-MS/MS technology. Process and analyze the data, including data correction, peak identification, and quantitative analysis to extract valuable drug properties information.
HT-ADME Screening Assay Portfolio
- Thermodynamic and kinetic measurements.
- Metabolic stability assays: including primary hepatocytes, microsomes (human or animal liver microsomes), and plasma (human or animal) stability tests.
- Permeability assays: including MDCK, Caco-2 cell lines, and 96-well high-throughput parallel artificial membrane permeability assay (PAMPA).
- Metabolite analysis and identification: analysis post-exposure to cells, tissues, plasma, or microsomes.
- Protein binding assays: including plasma, tissue, microsomes.
- Red blood cell partitioning assays.
Advantages of Creative Bioarray's HT-ADME Screening Services
- Flexible customization according to client needs, offering tailored services from basic ADME screening to in-depth metabolic mechanism research.
- High-throughput rapid screening with a leading platform and bioinformatics analysis system, ensuring accuracy and timeliness of results.
- Integration of in vitro screening with computational modeling for predictive models and decision support in drug discovery.
FAQ
1: How does high-throughput ADME screening differ from traditional methods?
High-throughput ADME screening differs from traditional methods in several ways. It employs automated systems, microplate formats, and sensitive detection instruments, enabling the simultaneous screening of millions of samples. This approach is faster, more efficient, and offers higher specificity. In contrast, traditional methods are often low-throughput, time-consuming, and require larger sample sizes, limiting their ability to handle large datasets.
2: Can customized services be provided according to our specific needs?
Yes, we offer bespoke ADME screening services, including specific drug targets and disease models to meet your needs.
3: How are HT-ADME screening results applied in drug development?
HT-ADME results offer critical insights into drug properties, metabolic pathways, and toxicity. These results guide structural optimization and candidate selection, and inform subsequent animal and clinical trial designs, accelerating drug development.
4: How to choose suitable compounds for HT-ADME screening?
Selecting suitable compounds is based on early-stage development needs and goals. Priority is given to candidates demonstrating drug potential during lead optimization. Assess compound complexity, metabolic pathways, and interactions to ensure relevant and effective results, saving resources and enhancing development success.
Quotation and Ordering
Leveraging our profound expertise and advanced technology, Creative Bioarray delivers reliable and economical HT-ADME assays, ensuring superior quality and consistent results. We offer tailored assay solutions to meet our clients' specific objectives. Reach out to us to learn more about how we can support your needs.
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