Potent and selective lysosomal acid lipase (LAL) inhibitor (IC50 = 68 nM). Exhibits no significant activity against pancreatic lipase or lipoprotein lipase at 10 μM concentration. Blocks LAL-mediated lipid hydrolysis of acetylated LDL and reduces efflux of cholesterol from lipid-loaded cells resulting in increased cellular cholesterol ester levels.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 298.36. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.35 mL||16.76 mL||33.52 mL|
|5 mM||0.67 mL||3.35 mL||6.7 mL|
|10 mM||0.34 mL||1.68 mL||3.35 mL|
|50 mM||0.07 mL||0.34 mL||0.67 mL|
References are publications that support the products' biological activity.
Rosenbaum et al (2009) Chemical screen to reduce sterol accumulation in Niemann-Pick C disease cells identifies novel lysosomal acid lipase inhibitors. Biochim.Biophys.Acta. 1791 1155 PMID: 19699313
Ouimet et al (2011) Autophagy regulates cholesterol efflux from macrophage foam cells via lysosomal acid lipase. Cell Metab. 13 655 PMID: 21641547
Rosenbaum et al (2010) Thiadiazole carbamates: potent inhibitors of lysosomal acid lipase and potential Niemann-Pick type C disease therapeutics. J.Med.Chem. 53 5281 PMID: 20557099
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