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Beschreibung

A cell-permeable thiosemicarbazone copper chelator that potently blocks the HDL receptor SR-BI- (scavenger receptor, class B, type I) mediated lipid uptake (IC50 = 21 and 57 nM against DiI and CE uptake, respectively, from DiI-HDL and CE-HDL using hamster ldlA-7 cells expressing murine SR-BI) in a reversible manner, while exerting little effect toward intracellular membrane trafficking or cytoskeletal organization. BLT-1 chelates Cu+2 in a 2:1 stoichiometric ratio and a half molar equivalent of CuCl2 is shown to fully prevent zebrafish embryos from BLT-1-induced development defects, while BLT-1 can likewise be used to chelate excess amount of copper (>4 µ,M) and rescue embryos from copper toxicity.