Orlistat

Catalog No.S1629 Batch:S162902

Technical Data

Formula	C₂₉H₅₃NO₅
Molecular Weight	495.73	CAS No.	96829-58-2
Solubility (25°C)*	In vitro	DMSO	99 mg/mL (199.7 mM)
		Ethanol	99 mg/mL (199.7 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Orlistat is a general lipase inhibitor with IC50 of 122 ng/ml for PL from human duodenal juice. Orlistat treatment reduces proliferation, induces apoptosis and arrests cell cycle.

Targets

lipase ^[1]
(Cell-free assay)

Fatty acid synthesis ^[1]
(Cell-free assay)

In vitro

Orlistat, an inhibitor of lipases and fatty acid synthase, is used orally for long-term treatment of obesity. Orlistat shows antiproliferative activity against cancer cells in vitro. It has been found to augment pro-apoptotic NOXA protein^[1].

In vivo

Orlistat, administered by oral route, is minimally absorbed by the gastrointestinal tract and is able to prevent the absorption of a large percentage of lipids, thereby reducing lipid supply from outside sources^[1]. Because of its extremely low oral bioavailability, the effects of Orlistat are largely confined to the gastrointestinal tract, where it inactivates pancreatic lipase. Therefore, the formulation and route of delivery would have to be changed to treat tumors of the breast, prostate, and so on. Orlistat halts tumor cell proliferation, induces tumor cell apoptosis, and inhibits the growth of PC-3 tumors in nude mice. A pharmacokinetic analysis of Orlistat (155 mg/kg) administered by i.p. injection showed peak blood levels to be ∼10 μM 2 h after dosing (data not shown). Beyond this time, blood levels of the drug decayed rapidly^[2].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Jurkat CD4+ T cell leukemia cell line Concentrations 2.5, 5, 10, 20, 40 μM Incubation Time 2 days Method Leukemic cells were cultured in the presence of graded concentrations of orlistat for two days. Control cultures were exposed to DMSO alone at the concentration corresponding to that utilized for orlistat 40 μM. At the end of the in vitro treatment, leukemic cells were lysed and subjected to western blot (WB) analysis.
Animal Study:^{^[2]}	Animal Models Nude mice (PC-3 xenograft tumor) Dosages 240 mg/kg/day Administration i.p.

Cell Assay:^{^[1]}

Cell lines
Jurkat CD4+ T cell leukemia cell line
Concentrations
2.5, 5, 10, 20, 40 μM
Incubation Time
2 days
Method
Leukemic cells were cultured in the presence of graded concentrations of orlistat for two days. Control cultures were exposed to DMSO alone at the concentration corresponding to that utilized for orlistat 40 μM. At the end of the in vitro treatment, leukemic cells were lysed and subjected to western blot (WB) analysis.

Animal Study:^{^[2]}

Animal Models
Nude mice (PC-3 xenograft tumor)
Dosages
240 mg/kg/day
Administration
i.p.

References

Selleck's Orlistat has been cited by 17 publications

Lipid droplet dynamics are essential for the development of the malaria parasite Plasmodium falciparum [ J Cell Sci, 2024, 137(20)jcs262162]	PubMed: 38962997
Histone malonylation is regulated by SIRT5 and KAT2A [ iScience, 2023, 26(3):106193]	PubMed: 36879797
Histone malonylation is regulated by SIRT5 and KAT2A [ iScience, 2023, 26(3):106193]	PubMed: 36879797
Inhibition, breast milk transmission and pancreatic tropism of SARS-CoV-2 [ OPARU, 2023, 10.18725/OPARU-48911]	PubMed: none
Gasdermin E mediates resistance of pancreatic adenocarcinoma to enzymatic digestion through a YBX1-mucin pathway [ Nat Cell Biol, 2022, 24(3):364-372]	PubMed: 35292781
Microglial hexokinase 2 deficiency increases ATP generation through lipid metabolism leading to β-amyloid clearance [ Nat Metab, 2022, 4(10):1287-1305]	PubMed: 36203054
Analysis of the metabolic proteome of lung adenocarcinomas by reverse-phase protein arrays (RPPA) emphasizes mitochondria as targets for therapy [ Oncogenesis, 2022, 11(1):24]	PubMed: 35534478
Controlling drug release by introducing lipase inhibitor within a lipid formulation [ Int J Pharm, 2022, 623:121958]	PubMed: 35760262
Activation of CTHRC1 by HOXB9 Promotes Angiogenesis through Fatty Acid Metabolism in Lung Adenocarcinoma [ Rev Invest Clin, 2022, 75(2):63-75]	PubMed: 37205792
Investigations into the use of enzyme inhibitors to control drug release for overdose prevention [ Monash University, 2022, ]	PubMed: None

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