Why put ANALIZA on your team for Blood Brain Barrier Permeability?
Analiza uses the LogD/LogK method for the prediction of a compound’s ability to permeate the blood-brain barrier. This method has a distinct advantage over techniques that rely on active kinetic measurements of permeability using model bilayers, since only equilibrium measurements are involved, and no complex artificial membranes are required. This validated method relies on a published set of correlations between LogP, measuring the relative affinity of a compound to lipid vs. water, together with LogK which quantifies the relative affinity of the compound to the different aqueous layers in plasma and the CNS fluid.
Our unique approach allows you test more compounds or test the same compounds at multiple pH levels. You no longer need to ration your BBB permeability data due to the high cost of complex experiments. Don’t leave your next blockbuster drug in the compound bank; test it today.
High Predictive Accuracy
- 96-100% for CNS+ compounds
Fast Turnaround Time
- Archival data returned electronically as early as 48 hours after receiving your compounds
Small Sample Requirement
- Typically 75µL of 30mM stock solution in DMSO
Inexpensive
- Fraction of the cost of PAMPA and Caco-2 assays
Universal Method of Detection
- Compound structure is not needed
- We only need to know the number of nitrogen atoms and molecular weight
Highest level of accuracy and repeatability
- Routinely performed complete calibration
- Real-time monitoring of all systems' critical performance parameters
- Each customer assay is performed with an on-board set of standards
Blood Brain Barrier Permeability Services Quick Facts
Assay: LogP/LogK relationship for prediction of passive blood brain barrier permeability.
Method: The probability of a CNS+ compound is determined using a relationship between octanol-water partition coefficient, LogD, to quantify the relative affinity of the compound to lipid vs. water phases, and a water-water partition coefficient, LogK, to quantify relative affinity to the different water structures representing blood and CSF. Both measurements are performed at pH 7.4. The experimental values of LogD and LogK are obtained using Analiza’s automated, miniaturized shake-flask methods and quantified using chemiluminescent total nitrogen detection. Method validation published in European Journal of Medicinal Chemistry (article available upon request).
LOD: -3<LogD<+4 (Nominal, actual compound-specific limits are determined by compound amount, molecular weight, and number of nitrogen atoms in each compound.
Accuracy: over 96% predicative accuracy for CNS+ and CNS- compounds, as validated against 63 literature compounds.
Source: DMSO dissolved compounds in 96 well plates, typically 75µL, 30mM concentration.
Turnaround time: As little as 48 hours, typically within 5 business days.
Results: Provided electronically. Tabulated data in Excel per customer instructions. All results are analyst-checked; internal standards included on each plate.
Experience: Developer of Automated ADME technologies since 1997 with tens of thousands of data points for clients ranging from large pharma to small biotechs.
