PROTAC Permeability Evaluation
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.
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.
- Parallel Artificial Membrane Permeability Assay (PAMPA)
Parallel artificial membrane permeability analysis (PAMPA) is a method for determining the entry of substances from the donor compartment into the recipient compartment through an artificial membrane injected with lipids. The donor uses a porous microtitration plate, and a membrane/receptor compartment is placed at the top, and the whole assembly is often referred to as a "sandwich". At the beginning of the test, the Protac® was added to the donor compartment, while the recipient compartment did not contain the drug. After a period of incubation that may include stirring, separate the sandwiches and measure the amount of the drug in each compartment.
- Madin-Darby Canine Kidney (MDCK) Permeability Assay
Madin-Darby canine kidney cell (MDCK) is a model mammal cell for biomedical research. MDCK cells are used in a wide range of cellular biological studies, including cell polarity, cell-to-cell adhesion (called adhesion junctions), collective cell movement, and responses to growth factors. Permeability analysis usually uses Madin-Darby canine kidney (MDCK) cells to predict intestinal absorption of Protac®.
- Caco-2 Permeability Assay
Caco-2 cell line is derived from human colon cancer. These cells have characteristics similar to intestinal epithelial cells, such as the formation of polarized monolayers, clear brush edges on the apical surface, and cell-to-cell connections. The outflow ratio, which provides an indicator of whether the compound has experienced active outflow, can be determined by evaluating the transport of the monolayer in two directions (tip-to-basal side (AmurB) and basal side-to-tip (BMel A). Caco-2 permeability is included in our portfolio of in vitro ADME screening services. BOC Sciences provides consistent, high-quality, and cost-effective data through a highly automated approach.
- One-stop Protac® service platform
- Extensive knowledge and experience in assay designing and data analyzing
- Experienced scientific team
- Advanced instruments and equipment
- Reliable and reproducible data
- 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.
- 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.
- 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.