Estimation of the unbound fraction of drug in brain provides a valuable tool in identifying new therapies for CNS diseases. For many years emphasis has been placed on the magnitude of the brain to plasma ratio (B/P ratio or Kp), even though, in many cases, brain total concentration correlates poorly with a mechanistic pharmacodynamic response. Total drug concentration values in brain, measured in vivo experiments or estimated with the hybrid model supplied with TRANSIL Brain Absorption kit plus are corrected for the fraction of drug unbound estimated by the TRANSIL Brain Absorption kit to obtain an estimate of the brain unbound concentration (Cu,brain). This has been successfully demonstrated across a range of CNS targets to yield a much better correspondence with receptor occupancy and pharmacodynamic endpoints.
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Products
Liver Microsomal Binding (fu mic)
Our TRANSIL Fu Mic kit evaluates the free fraction of drug candidates in metabolic stability incubations with liver microsomes. The kit assesses the drugs affinity to membranes of liver microsomes and directly calculates the free fraction in the incubation. Due to the short incubation time of only 12 minutes the kit is not only a fast high-throughput assay, it also minimizes the effect of compound stability issues.
Advantages of TRANSIL:
To order your protein binding kits contact orders@sovicell.com.
