For drug discovery laboratories seeking increased ADME compound profiling throughput, Transil sample preparation microplates provides automated methods through the combination of beads pre-dispensed in a microplate format.
The Transil Membrane Affinity assay provides data that correlates better to in vivo studies compared to the more conventional water/octanol partitioning assays because it uses beads which are coated with a lipid bilayer that mimic interactions between compounds and cell membranes. The results are equivalent to the liposome "gold standard" method, without the tedious preparation of liposomes.
The Transil HSA Binding assay kit makes routine, high-throughput HSA binding characterisation easy as it contains beads, which have been coated with human serum albumin and pre-dispensed into a microplate format. The pre-dispensed format increases throughput via parallel sample preparation and assay reading on Molecular Devices' SpectraMax microplate readers.
Transil Human Serum Albumin (HSA) binding assays characterise blood protein binding properties by measuring the fraction bound to Human Serum Albumin. Transil HSA consists of covalently bound Human Serum Albumin immobilised on an inert and soft surface. Non-specific interactions between compounds and the immobilisation layer are minimised by design. Pharmacologically important binding sites are freely accessible.
The design of the assay kit ensures that the experimental process is kept as simple as possible. The process involves adding compounds to the plate, mix, separate beads from supernatant, and read on UV-Vis microplate readers or LC/MS systems. Data reduction routines are included to ensure rapid methods start-up and accurate data reduction.
With the Transil assays, there is virtually no methods development required, as each kit contains data analysis routines for processing high-throughput screening of drug candidates for early ADME characterisation. Furthermore, the assays share nearly identical sample workup steps, so steps developed for one assay are immediately applicable to the other.
"The Transil assay kits enable screening of compound libraries for membrane affinity and HSA binding for early ADME properties which are not possible with current low-throughput methods," Christopher Silva, director of marketing for life sciences products at Molecular Devices stated.
"These new assays require only one sample concentration, which simplifies automation. Additionally, turnkey data analysis offers researchers compound data within hours of synthesis or secondary screening."
The kits are available in two formats for 96- or 384-well microplates. The "high precision" version is ideal for profiling compounds at the lead optimisation stage of drug discovery; the "high throughput" version allows characterisation of compound libraries.