Key result
U-57,908 (RHC 80267) inhibited lipoprotein lipase activity in rat cardiac myocytes, requiring concentrations of 1.1 microM and 2.5 microM for 50% inhibition in homogenates and post-heparin medium.
U-57,908 is a potent and selective LPL inhibitor that may provide a useful experimental approach in studies on lipoprotein metabolism.
May aid experimental LPL inhibition studies in cardiac models; leaves open any clinical translation in humans.
U-57,908 (RHC 80267) was shown to inhibit lipoprotein lipase (LPL) activity in cardiac myocytes from rat hearts; the concentrations required for inhibition to 50% of control activity were 1.1 microM and 2.5 microM for myocyte homogenates and a post-heparin medium preparation, respectively. The inhibition of LPL activity by U-57,908 was not changed when the concentration of the triolein substrate and apolipoprotein CII activator in the assay was reduced. The availability of U-57,908 as a potent and selective LPL inhibitor may provide a useful experimental approach in studies on lipoprotein metabolism.
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Carroll et al. (1992) studied this question. U-57,908 (RHC 80267) vs. control activity was evaluated on lipoprotein lipase (LPL) activity inhibition to 50% of control activity. U-57,908 (RHC 80267) inhibited lipoprotein lipase activity in rat cardiac myocytes, requiring concentrations of 1.1 microM and 2.5 microM for 50% inhibition in homogenates and post-heparin medium.
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