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Custom synthesis service for fluorescent ligands
Celtarys provides custom chemical development services, specifically for the identification of a broad range of robust and complex fluorescent ligands not commercially available for the majority of therapeutic targets.
Thanks to our LEGO-like chemical conjugation technology, we can offer a portfolio of custom development extremely varied of polyfunctional fluorescent ligands.
Fluorescent ligands are composed of a pharmacophore, that specifically recognizes the target, and a fluorophore, connected by a linker. The linker has a significant influence on the biological activity of such conjugates and its nature and length play a critical role in the physicochemical properties and bioactivity of the whole final conjugate.
Thanks to our proprietary patented synthetic technology named LEGO-like chemical conjugation, we can develop tailor-made fluorescent ligands for any target of interest. Our semi-combinatorial technology allows us to design hundreds of different chemical linkers architectures, accelerating the development process and improving synthesis outcomes.
Moreover, most of the fluorophore chemical classes are compatible with our synthetic strategy thus allowing to spread of the applicability of the optimized fluorescent ligands in different assays (Fluorescence Polarization, HTRF, High Content Screening, confocal imaging, flow cytometry…).
OUR APPROACH
PHASE 1
We start with the identification of the appropriate pharmacophore(s) for each target, using an integrated approach that includes both structure-based and ligand-based drug design approaches for compound functionalization. Thanks to in-silico experimental structure-activity study we identify the optimal position for pharmacophore functionalization and linker conjugation. The optimal pharmacophore(s) are typically identified among a set of 3-5 different chemical scaffolds.
PHASE 2
Once identified the functionalized pharmacophore with the best physicochemical and pharmacological profile, we prepare a library of intermediates (pharmacophore + linker) using our own LEGO-like chemical conjugation technology. The biological evaluation of these compounds allows us to identify the optimal linker(s) for the target of interest and for the desired application.
PHASE 3
In the last phase, we combine the previous identified precursors with fluorophores suitable for the kind of assay of interest. The activity of the final molecules, measured in a binding or functional assay, allows us to select the best one(s).
HOW TO START A PROJECT WITH US?
Are you interested to explore our custom development services for a fluorescent ligand of your interest?
Let us know some more detail about your project, by answering the following questions:
- Which is the target of your interest?
- The fluorescent ligand will be used for in vivo or in vitro experiments?
- Are you going to use fixed or living cells?
- Are you going to use native or transfected cells?
- Are you going to use it in 2D (cell plates) or 3D cell structures (e.g. spheroids)?
- What type of organism are you going to study (i.e: mouse, human)?
- In which kind of assay are you going to use the fluorescent probe to be developed (i.e: Flow cytometry, High content screening, Fluorescent Polarization, etc)?
- Have you any specific requirements of wavelength ranges for excitation/emission of the fluorophore?
