| Name | Orlistat |
| Description | Orlistat (Tetrahydrolipstatin) is a lipase inhibitor and a fatty acid synthase (FASN) inhibitor. Orlistat has been shown to promote weight loss. |
| In vitro | METHODS: Prostate cancer cells PC3, DU145 and LNCaP were treated with Orlistat (10-300 µM) for 24 h and cell proliferation was detected by MTT assay.
RESULTS: Increasing concentrations of Orlistat resulted in a dose-dependent decrease in cell viability of the three PCa cell lines tested. [1]
METHODS: Breast cancer cells SK-Br3 were treated with Orlistat (40 µM) for 6-72 h. Cell cycle was measured by Flow cytometry.
RESULTS: The time-dependent response of SK-Br3 breast cancer cells to Orlistat was characterized by the absence of G2-M populations and the accumulation of cells in the S phase of the cell cycle. Importantly, Orlistat exposure significantly promoted apoptosis, as evidenced by the time-dependent accumulation of sub-G1 populations with <2N DNA and representing dead cells. [2] |
| In vivo | METHODS: To detect anti-tumor activity in vivo, Orlistat (240 mg/kg, 33% ethanol and 66% PEG 400) was injected intraperitoneally into athymic nude mice bearing PC-3 xenografts once daily for three weeks.
RESULTS: Orlistat prevented PC-3 tumor growth. In five separate experiments, tumor growth was blocked by 63%, 62%, 46%, 41%, and 16%. [3] |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 45 mg/mL (90.78 mM), Sonication is recommended.
Ethanol : 49.6 mg/mL (100.05 mM), Sonication is recommended.
33% Ethanol + 67% PEG 400/PEG 300 : 10 mg/mL (20.17 mM), In vivo: Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
|
| Keywords | triacylglycerol lipase | synthase | pancreatic | Orlistat | oncogene | metabolic | lipases | Inhibitor | inhibit | gastric | FattyAcidSynthase | Fatty Acid Synthase (FASN) | Fatty Acid Synthase | fatty | FASN | FAS | atherosclerotic | Apoptosis | Anti-obesity | acid |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Acetylcysteine | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | L-Glutamic acid | Metronidazole | Tributyrin | L-Ascorbic acid sodium salt | Salicylic acid |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Drug Library | Anti-Cancer Approved Drug Library | Anti-Aging Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
United States
