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Beschreibung

A cell permeable thioxothiazolindine compound that reversibly inhibits FATP2-mediated long chain fatty acid uptake in Caco-2 and HepG2, but not non-FATP2-expressing 3T3-L1 adipocytes, cultures (IC50 = 3.99, 7.55, and 231.1 µ,M, respectively), while exhibiting much reduced potency toward cellular Acsl (acyl-CoA synthetase) activity (IC50 = 50 µ,M). Shown not to affect Caco-2 viability, membrane permeability, or glucose transport., A cell permeable thioxothiazolindine compound that reversibly inhibits FATP2- (fatty acid transport protein 2) mediated long chain fatty acid uptake in Caco-2 and HepG2, but not non-FATP2-expressing 3T3-L1 adipocytes, cultures (IC50 against C1-BODIPY-C12 = 3.99, 7.55, and 231.1 µ,M, respectively), exhibiting much reduced potency toward cellular Acsl (acyl-CoA synthetase) activity (IC50 = 50 µ,M using lysates from 1h inhibitor-treated Caco-2 cells). Shown not to affect Caco-2 viability (50 µ,M in MTT assay), membrane permeability (by trans-epithelial electrical resistance measurement, 50 µ,M), glucose transport (20 µ,M in 2-NBDG uptake assay).