Orlistat

SKU: orb1310386

Description

Orlistat, also known as Tetrahydrolipstatin, is a small molecule that inhibits both lipase and fatty acid synthase (FASN). This dual mechanism underlies its application in obesity research, where it is used in vitro and in vivo to study lipid metabolism and promote weight loss.

Research Area

Cell Biology, Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 96829-58-2
• MW: 495.75
• Purity: >98%
• Formula: C₂₉H₅₃NO₅
• SMILES: C([C@@H](OC([C@H](CC(C)C)NC=O)=O)CCCCCCCCCCC)[C@H]1[C@H](CCCCCC)C(=O)O1
• Target: Lipase
• Solubility: Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 50 mg/ml).

Bioactivity

• 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%.
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• 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. 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ro18-0647; Tetrahydrolipstatin (-)

Compound Identifiers

PubChem CID

3034010