Inhibition of myocardial lipoprotein lipase by U-57,908 (RHC 80267).
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.
Carroll
R
R
MRC Signal Transduction Group, Faculty of Medicine, University of Calgary, Alberta, Canada.
Severson
D L
DL
D000818:Animals; D003512:Cyclohexanones / Q000494:pharmacology*; D066298:In Vitro Techniques; D008071:Lipoprotein Lipase / Q000037:antagonists & inhibitors*; D008297:Male; D009206:Myocardium / Q000201:enzymology*; D051381:Rats; D011919:Rats, Inbred Strains; D014304:Triolein / Q000494:pharmacology; D014316:Tritium
D003512:Cyclohexanones; D014316:Tritium; D014304:Triolein; C036535:1,6-bis(cyclohexyloximinocarbonyl)hexane; D008071:Lipoprotein Lipase