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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. 了解 Tocris 化合物库的更多信息。
分子量 | 298.36 |
公式 | C12H18N4O3S |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 501104-16-1 |
PubChem ID | 648404 |
InChI Key | GKOPFXFKPASEFI-UHFFFAOYSA-N |
Smiles | O=C(OC1=NSN=C1N2CCCCC2)N3CCOCC3 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 29.84 | 100 | |
ethanol | 29.84 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
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引用文献是使用了 Tocris 产品的出版物。 Lalistat 1 的部分引用包括:
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
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
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