Orlistat

Catalog No.S1629 Batch:S162903

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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.

Selleck's Orlistat has been cited by 14 publications

Histone malonylation is regulated by SIRT5 and KAT2A [ iScience, 2023, 26(3):106193] PubMed: 36879797
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
Pharmacological inhibition of fatty acid synthesis blocks SARS-CoV-2 replication [ Nat Metab, 2021, 10.1038/s42255-021-00479-4] PubMed: 34580494
LINC00842 inactivates transcription co-regulator PGC-1α to promote pancreatic cancer malignancy through metabolic remodelling [ Nat Commun, 2021, 12(1):3830] PubMed: 34158490
Brown adipocyte ATF4 activation improves thermoregulation and systemic metabolism [ Cell Rep, 2021, 36(12):109742] PubMed: 34551310

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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