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Submit ReviewLalistat 1 is a 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.
Lalistat 1 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
M. Wt | 298.36 |
Formula | C12H18N4O3S |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 501104-16-1 |
PubChem ID | 648404 |
InChI Key | GKOPFXFKPASEFI-UHFFFAOYSA-N |
Smiles | O=C(OC1=NSN=C1N2CCCCC2)N3CCOCC3 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 29.84 | 100 | |
ethanol | 29.84 | 100 |
The following data is based on the product molecular weight 298.36. Batch specific molecular weights may vary from batch to batch due to the degree 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 biological activity of the product.
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
If you know of a relevant reference for Lalistat 1, please let us know.
Keywords: Lalistat 1, Lalistat 1 supplier, potent, selective, LAL, inhibitors, inhibits, lysosomal, acid, lipase, Neimann-Pick, type, c, NPC, storage, cholesterol, accumulation, Lalistat1, Lysosomal, Acid, Lipase, (LAL), 6098, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Lalistat 1 include:
Wu et al (2019) Evidence for a Novel Regulatory Interaction Involving Cyclin D1, Lipid Droplets, Lipolysis, and Cell Cycle Progression in Hepatocytes. Hepatol Commun 3 406 PMID: 30859152
Shaun G et al (2019) Lipid droplet size directs lipolysis and lipophagy catabolism in hepatocytes. J Cell Biol 218 3320-3335 PMID: 31391210
Mariam et al (2021) Lipophagy-derived fatty acids undergo extracellular efflux via lysosomal exocytosis. Autophagy 17 690-705 PMID: 32070194
Do you know of a great paper that uses Lalistat 1 from Tocris? Please let us know.
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