PROTAC Permeability Evaluation

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* Please be kindly noted that our services and products can only be used for research to organizations or companies and not intended for any clinical or individuals.

As a recognized leader in the field of drug discovery and development, BOC Sciences is committed to the development of Protac®, we provide our customers with a comprehensive cell permeability assay services. All BOC Sciences absorption and penetration analysis can be used in standard human and animal model systems and can be ordered individually, in combination, or as a range of key services provided in candidate drug evaluation kits to save costs.

Introduction

The degree and character of intestinal tract absorption is an important factor that affects the bioavailability of oral drugs. Passive diffusion through the cell membrane is a key factor in cross-cellular absorption, which is also the way in which most drugs are absorbed (paracellular absorption and active transport are other pathways). The processes of dissolution, diffusion, and resolution required for passive infiltration of cell membranes are functions of the properties of compounds, including size, polarity, lipophilicity, and conformational kinetics. In the early stage of discovery and development, it is necessary to screen the cell osmotic efficiency of candidate drugs in order to evaluate their absorptive potential.

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References:

  1. Moreau, K., Coen, M., Zhang, A. X., Pachl, F., Castaldi, M. P., Dahl, G., ... & Newham, P. (2020). Protac® (PROteolysis TArgeting Chimeras) in drug development: a safety perspective. British Journal of Pharmacology.
  2. van Breemen, R. B., & Li, Y. (2005). Caco-2 cell permeability assays to measure drug absorption. Expert opinion on drug metabolism & toxicology, 1(2), 175-185.
  3. Bennion, B. J., Be, N. A., McNerney, M. W., Lao, V., Carlson, E. M., Valdez, C. A., ... & Carpenter, T. S. (2017). Predicting a drug's membrane permeability: A computational model validated with in vitro permeability assay data. The Journal of Physical Chemistry B, 121(20), 5228-5237.

* PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

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