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Orlistat

Orlistat is an inhibitor of fatty acid synthase that is clinically administered for its anti-obesity benefits. Orlistat is often used as a weight loss aid, although it also exhibits anticancer chemotherapeutic activity. In animal models of T cell lymphoma, orlistat increases levels of ROS, NO, caspase 3, Bcl-2, and p53, increasing life span and inhibiting tumor growth; similar results are found in animal models of colorectal carcinoma.

References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18951053

Cas No.

96829-58-2

Purity

≥98%

Formula

C29H53NO5

Formula Wt.

495.73

Chemical Name

N-Formyl-L-leucine(1S)-1-[[(2S,3S)-3-hexyl-4-oxo-2-oxetanyl]methyl]-dodecyl ester

IUPAC Name

(2S)-1-[(2S,3S)-3-Hexyl-4-oxo-2-oxetanyl]-2-tridecanyl N-formyl-L-leucinate

Synonym

Orlipastat; Xenical

Melting Point

43°C

Solubility

Soluble in DMSO or ethanol.

Appearance

Off-white waxy powder

Kant S, Kumar A, Singh SM. Tumor growth retardation and chemosensitizing action of fatty acid synthase inhibitor orlistat on T cell lymphoma: implication of reconstituted tumor microenvironment and multidrug resistance phenotype. Biochim Biophys Acta. 2014 Jan;1840(1):294-302. PMID: 24060750.

Chuang HY, Chang YF, Hwang JJ. Antitumor effect of orlistat, a fatty acid synthase inhibitor, is via activation of caspase-3 on human colorectal carcinoma-bearing animal. Biomed Pharmacother. 2011 Jul;65(4):286-92. PMID: 21723078.

Halpern A, Pepe RB, Monegaglia AP, et al. Efficacy and tolerability of the association of sibutramine and orlistat for six months in overweight and obese patients. J Obes. 2010;2010. pii: 602537. PMID: 20871858.

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