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Biology Chemistry DMPK Pharmacology Toxicology

Plasma Stability

Service Description

Provider: BioFocus DPI is the service division of Galapagos NV. BioFocus DPI offers a comprehensive suite of discovery products and services. These are available separately or as an integrated drug discovery solution, backed by a centralized project management system.

Background: Certain classes of drug are potentially labile to the enzymes contained in plasma, structures containing ester or amide linked groups are at higher risk of metabolism by esterase, amidase or protease enzymes. Screening higher risk compounds prior to plasma protein binding assays or in vivo sample collection minimizes the chance of unpredictable results due to in sample degradation of the analyte. Plasma instability may be desirable in programs using a pro-drug approach.

Service Details: Incubations of test compounds (5 µM initial concentration, n=2) are carried out with neat plasma. The incubations are performed at 37°C with aliquots taken at 0, 15, 30, 60 and 120 minutes, and reactions terminated by addition of acetonitrile containing analytical internal standard. Samples are centrifuged and the supernatant fractions analyzed by LC-MS/MS. The instrument responses (peak heights) are referenced to the zero time-point samples (as 100%) in order to determine the percentage of compound remaining. Ln plots of the % remaining for each compound are used to determine the half-life for the plasma incubations. Half-life values are calculated from the relationship T1/2 = -0.693/lambda, where lambda was the slope of the concentration vs. time curve. Standard compounds, simvastatin and eucatropine, are included to provide an indication of the metabolic capacity of the plasma with respect to esterase activity.

Deliverable: Assay results together with details of the assay methodology, analytical methods used and quality control data are reported. A full interpretation of the results obtained are provided. Where available, these results will be compared to other data for the compound/series and recommendations made as to further experiments or analysis which may be of value from an ADME perspective.

Price: The listed price is applicable for a batch of 10-19 compounds at $400 per compound per species. For other batch sizes or assay formats please request a quotation by clicking on the orange ‘Request Info’ button.

Sample Submission: Enter sample submission information and select service options in the Service Order Form that you can access once you add this item to your cart. Please submit a minimum of 10 µL of a 10 mM solution in DMSO. Compounds can be supplied in 96 well format or in vials. If providing solid, please supply approximately 1mg (accurately weighed). The default solvent is DMSO and compound stocks will be stored at – 20°C unless otherwise advised. Provision of structures is desirable, but not essential. Our quality service and expertise can best be demonstrated when structures are supplied as this assists in our interpretation of the results obtained.

How To Get Info

Click on the orange 'Request Info' button to request a custom quote, get bulk discount pricing, ask technical questions or request a meeting. Once you submit your request, you can communicate with the provider or exchange files by using Assay Depot’s microblogging system.

How To Order

Click on the orange 'Add to Cart' button to access the Service Order Form, which contains technical questions and sample submission information. The form allows you to type in or paste in information or to select from a list of pre-defined choices. Complete and submit the Service Order Form to start the checkout process.

Once you submit your order, you can communicate with the provider or upload files by using Assay Depot’s microblogging system. The microblogging system allows you to stay in direct contact with the provider the entire time a research service is being carried out.


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