Cell permeable, irreversible inhibitor of gastric and pancreatic lipases. Shows only minimal activity against amylase, trypsin, chymotrypsin, or phospholipase A2 (PLA2). Partially inhibits the hydrolysis of triglycerides and lowers the absorption of dietary fat and promotes weight loss. Anti-obesity drug. Exhibits antitumor activity by inhibition of the thioesterase domain of fatty acid synthase (FAS) both in vitro and in vivo.
Product Details
| Alternative Name: | Tetrahydrolipstatin, N-Formyl-L-leucine-(1S)-1-(((2S,3S)-3-hexyl-4-oxo-2-oxetanyl)methyl)dodecyl ester |
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| Formula: | C29H53NO5 |
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| MW: | 495.7 |
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| Source: | Synthetic. Originally isolated from Streptomyces sp. |
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| CAS: | 96829-58-2 |
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| MI: | 14: 6869 |
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| Purity: | ≥97% |
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| Appearance: | White to off-white solid. |
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| Solubility: | Soluble in DMSO or 100% ethanol. |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| Use/Stability: | Stock solutions are stable for up to 6 weeks when stored at -20°C. |
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| Handling: | Protect from light and moisture. After reconstitution, prepare aliquots and store at -20°C. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Orlistat and sibutramine beyond weight loss: E. Mannucci, et al.; Nutr. Metab. Cardiovasc. Dis.
70, 1228 (2008),
Abstract;
Antitumoral actions of the anti-obesity drug orlistat (XenicalTM) in breast cancer cells: blockade of cell cycle progression, promotion of apoptotic cell death and PEA3-mediated transcriptional repression of Her2/neu (erbB-2) oncogene: J.A. Menendez, et al.; Ann. Oncol.
16, 1253 (2005),
Abstract;
Differential uptake of subfractions of triglyceride-rich lipoproteins by THP-1 macrophages: A.M. Palmer, et al.; Atherosclerosis
180, 233 (2005),
Abstract;
A fatty acid synthase blockade induces tumor cell-cycle arrest by down-regulating Skp2: L.M. Knowles, et al.; J. Biol. Chem.
279, 30540 (2004),
Abstract;
Full Text
Orlistat is a novel inhibitor of fatty acid synthase with antitumor activity: S.J. Kridel, et al.; Cancer Res.
64, 2070 (2004),
Abstract;
Degree of in vivo inhibition of human gastric and pancreatic lipases by Orlistat (Tetrahydrolipstatin, THL) in the stomach and small intestine: B. Sternby, et al.; Clin. Nutr.
21, 395 (2002),
Abstract;
Interactions of lipoprotein lipase with the active-site inhibitor tetrahydrolipstatin (Orlistat): A. Lookene, et al.; Eur. J. Biochem.
222, 395 (1994),
Abstract;
