Orlistat

ALX-350-152

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Fatty acid synthase inhibitor

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.

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Product Details

Alternative Name	Tetrahydrolipstatin, N-Formyl-L-leucine-(1S)-1-(((2S,3S)-3-hexyl-4-oxo-2-oxetanyl)methyl)dodecyl ester
Appearance	White to off-white solid.
CAS	96829-58-2
Couple Target	Fatty acid synthase
Couple Type	Inhibitor
Formula	C₂₉H₅₃NO₅
MI	14: 6869
MW	495.7
Purity	≥97%
Solubility	Soluble in DMSO or 100% ethanol.
Source	Synthetic. Originally isolated from Streptomyces sp.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Stock solutions are stable for up to 6 weeks when stored at -20°C.
Handling	Protect from light and moisture. After reconstitution, prepare aliquots and store at -20°C.
Long Term Storage	-20°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

Integration of multi-modal measurements identifies critical mechanisms of tuberculosis drug action: Johnson, W. C., Alivisatos, A., et al.; Cell Syst. 16, 101348 (2025), Abstract
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

Last modified: May 29, 2024

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Orlistat

ALX-350-152

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