In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml
Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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.)
Preparing Stock Solutions
Biological Activity
Description
Orlistat is a general lipase inhibitor with IC50 of 122 ng/ml for PL from human duodenal juice. This compound treatment reduces proliferation, induces apoptosis and arrests cell cycle.
Targets
lipase (Cell-free assay)
Fatty acid synthesis (Cell-free assay)
In vitro
Orlistat, an inhibitor of lipases and Fatty Acid Synthase, is used orally for long-term treatment of obesity. This compound shows antiproliferative activity against cancer cells in vitro. It has been found to augment pro-apoptotic NOXA protein.
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. Because of its extremely low oral bioavailability, the effects of this compound 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 tumours of the breast, prostate, and so on. This chemical halts tumour cell proliferation, induces tumour cell apoptosis, and inhibits the growth of PC-3 tumours in nude mice. A pharmacokinetic analysis of this compound (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.
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 this compound 40 μM. At the end of the in vitro treatment, leukemic cells were lysed and subjected to western blot (WB) analysis.
Acyl-CoA thioesterase 8 induces gemcitabine resistance via regulation of lipid metabolism and antiferroptotic activity in pancreatic ductal adenocarcinoma
[ Acta Pharmacol Sin, 2025, 10.1038/s41401-025-01477-y]
Microglial hexokinase 2 deficiency increases ATP generation through lipid metabolism leading to β-amyloid clearance
[ Nat Metab, 2022, 4(10):1287-1305]
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]
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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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