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Radiopharmaceutical Blocking Assay Services

Rdcthera is a reputed organization engaged in providing integrated in-vitro blocking assay services for radiopharmaceuticals. State-of-the-art services have been designed by us to assess saturability and specificity patterns of binding of radiopharmaceuticals to their targeted sites of action, thereby creating valuable information for drug development and research.

Understanding Blocking Assay

These assays are indispensable for the assessment of specificity and saturability of radiopharmaceutical binding to a target. In such experiments, a competing, unlabelled ligand is introduced to bind to the target, reducing or blocking the binding of the radiopharmaceutical tracer. By doing this, we can actually profile the specificity of the tracer and identify off-target interactions. This validation is important to ensure the binding of the radiopharmaceutical to the target of interest only, so enhancing accuracy and effectiveness in diagnostic and therapeutic applications.

Fig 1. Blocking assay. Fig. 1. Cell uptake and blocking assay. (Pan Y, et al., 2019)

Our Radiopharmaceutical Blocking Assay Services

Rdcthera provides clients with a wide selection of radiopharmaceutical blocking assay services tailored to the client's needs. Our team of professionals brings a wealth of experience, current techniques, state-of-the-art equipment, and up-to-date tools to conduct accurate and reliable blocking studies detailing in-depth analyses into the binding properties of radiopharmaceuticals.

  • Competitive Binding Assays
Testing the tracer's selectivity by adding competing ligands.
  • Saturability Studies
Demonstrating radiopharmaceuticals bind to specific targets through excess unlabelled ligands.
  • Off-Target Binding Analysis
Methods of eliminating possible off-target interactions to obtain biomechanism with high specificity.

Experimental Methods

Our blocking assays services are then conducted with very rigorous protocols and methodologies so that results are accurate and reproducible. This would involve fractionated extracts from expressed target cells, such as membrane homogenates or tissue slices, to assess selectivity for binding at the intended target in the presence of off-target signals.

  • Membrane Homogenates and Tissue Slices - Study of the binding selectivity using real tissue from the target region, in a biologically relevant environment.
  • Equilibrium Binding Studies - The radiopharmaceutical and blocking ligand should be at binding equilibrium to measure the characteristics of binding.
  • High Molar Concentration of Ligands - Resorting to blocking ligands only when their concentration would occupy at least 90% of target binding sites to avoid off-target effects.

Applications of In Vitro Autoradiography

Such studies have wide applications in the development of radiopharmaceuticals and research. The saturability and specificity of the binding can be evaluated in blocking studies, which is very important for establishing efficacy and safety in the use of radiopharmaceuticals in clinics.

  • Diagnostic Imaging
  • Therapeutic Radiopharmaceuticals
  • Drug Development

For more information on our radiopharmaceutical blocking assay services and to discuss your needs, please do not hesitate to contact us. We are very excited to have the opportunity to work with you in the development of breakthrough radiopharmaceuticals.

Reference

  1. Pan Y, Yang Z, Xu Y, et al. (2019). Targeting HER2-positive gastric cancer with a novel 18F-labeled ZHER2:342 probe. RSC Adv. 9(19):10990-10998.
For research use only. Not intended for any clinical use.

Rdcthera RDC

Rdcthera offers efficient, customized, and professional R&D services related to radionuclide drug conjugates.

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