Fast High-Throughput Assay for Brain Tissue Binding

An off the shelf high-throughput assay kit for brain tissue binding and brain disposition.

Brain Tissue Binding Assay

The TRANSIL Brain Absorption kit estimates the binding of drugs to brain tissue and predicts the disposition of drugs into the brain. Developed in cooperation with GSK, it measures the affinity of drugs to reconstituted porcine brain membranes. The brain membrane affinity is used to estimate the brain tissue binding and to predict the brain-to-plasma distribution via a hybrid model that also incorporates the drug’s polar surface area and it’s plasma protein binding.

TRANSIL Brain Absorption Kit

The kit consists of ready-to-use 96-well microtiter plates. One plate can be used for measuring brain tissue binding and brain disposition of up to 12 compounds. The assay requires only 5 steps: (i) addition of drug candidate, (ii) mixing and incubation for 12 minutes, (iii) removal of beads by centrifugation, (iv) sampling of supernatant, and (v) quantification of a drug candidate.

Capabilities

Detection system:

• LC/MS/MS
• Scintillation counting
• Others

Parameters estimated and predicted:

• Unbound fraction of drug in brain
• Brain-to-plasma distribution

Features & Benefits of the Brain Tissue Binding Assay kits

• Fast, requires only 20 minutes total assay time
• Measures brain tissue binding and predicts blood-brain barrier penetration
• Off-the-shelf format in 96-well plate format generating highly reproducible results
• Rapid compound quantification due to immobilized brain membranes
• Kit includes a spreadsheet for calculation of final results and traffic light system for data quality rating

For more information please contact Sovicell today.

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