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High-throughput Determination of aqueous solubility, precipitation or colloidal aggregate formation in small molecule screening sets
Introduction:
Determining the aqueous solubility of a compound is an essential parameter in drug discovery. Poor water solubility can interfere with in vitro testing, giving rise to inaccurate and irreproducible data. Compounds with low aqueous solubility tend to be highly bound to plasma proteins with poor systemic tissue distribution and increased potential of CYP-mediated drug inhibition. Another caveat to in vitro testing in aqueous systems is false-positives in bio-assays due to the formation of colloidal aggregates. Compounds that form these aqueous aggregates are found experimentally to be promiscuous inhibitors that act non-competitively and exhibit little to no structure-activity relationships. Aggregate formation occurs when individual molecules group together to form particles 30-1000 nm in diameter, and these aggregates behave as the active inhibitory species. This is a key problem in HTS studies which consumes valuable R&D dollars and must be identified early in the discovery phase to remove them from further testing.
ASDI offers solubility determination in aqueous systems. Linear serial dilutions of each compound to be analyzed are prepared in aqueous buffer at a specified pH. The assay is performed using a commercially available flow cytometer modified to determine particle precipitation via simultaneous analysis of multiple particle size ranges in high-throughput 96-well or 384-well formats.
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