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Beschreibung

A cell-permeable quinolinyl-benzenesulfonamide compound that acts as a potent reversible inhibitor against tissue-nonspecific (TN) alkaline phosphatase (AP) activity (IC50 = 190 nM) with CYP2C19 being the only other known target, while exhibiting little or no inhibitory activity in over 250 assays involving other enzymes, including, but not limited to, placental and intestinal APs (IC50 >100 microM), PHOSPHO1 phosphatase, and NPP1 phosphodiesterase. Kinetic studies indicate that the inhibition is uncompetitive with respect to the phosphate donor substrate and noncompetitive with respect to the acceptor substrate, indicating an allosteric inhibition mechanism. Subcutaneous dosing in rats in vivo is reported to result in plasma inhibitor concentrations in the therapeutic range (Cmax = 1.5 microg/ml 1 hr after 4.13 mg/kg by s.c.).