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3,3-Diphenylpropylamido-indocyanine sulfonamide.


Rajopadhye M.


Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013.
2006 Dec 13 [updated 2007 Jan 26].


Near infrared fluorophores (NIRF), described for in vivo fluorescence imaging of disease (1, 2) have been generally classified into nonspecific enhancers (e.g. ICG (3)), molecularly targeted fluorochromes (e.g. RGD-Cy (4, 5) or enzyme activatable agents (e.g. cathepsin sensitive NIRF probes) (6). These agents have shown great potential for invivo imaging of specific molecular targets, biological processes and cells (7). Specific fluorophores have been used to image angiogenesis, apoptosis, protease activity, receptor status, macrophage activity and to track cells (2, 8). Most of the affinity agents developed to date have molecular weights in excess of several thousand to millions (6, 9-11) to carry affinity ligands and/or to allow efficient quenching/de-quenching in large molecular weight constructs. Small molecule fluorophores with affinity to albumin could potentially exhibit an increase in fluorescence upon binding; thus a family of “activatable” fluorophores could be developed that consequently would provide enhanced or superior in vivo target-to-background ratios in live animals. As proof-of-principal, VM315, an NIRF containing a 3,3-diphenylpropyl moiety that provides a structural feature capable of non-covalent albumin binding was developed and tested. Those studies showed that VM315 exhibited a remarkable increase in fluorescence upon albumin binding (12). Such a molecule might be used to improve the detection of small cancers in vivo. Given the established role of fluorescent albumins in studying microvascular permeability in disease processes, VM315 may potentially represent a viable option for obtaining similar measurements clinically.

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