Orlistat

SKU: orb1223504

Description

Orlistat is a drug designed to treat obesity. Its primary function is preventing the absorption of fats from the human diet, thereby reducing caloric intake. Orlistat works by inhibiting pancreatic lipase, an enzyme that breaks down triglycerides in the intestine. Without this enzyme, triglycerides from the diet are prevented from being hydrolyzed into absorbable free fatty acids and are excreted undigested.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 96829-58-2
• MW: 495.73
• Purity: >98% (HPLC)
• Formula: C₂₉H₅₃NO₅
• SMILES: CC(C)C[C@H](NC=O)C(O[C@@H](CCCCCCCCCCC)C[C@@H]([C@@H]1CCCCCC)OC1=O)=O
• Target: Fatty Acid Synthase
• Solubility: Ethanol: 99 mg/mL (199.7 mM); DMSO: 99 mg/mL (199.7 mM)

Bioactivity

• In Vivo:
  Animal model: Eighteen male rats of Sprague–Dawley strain aged between 8–10 weeks weighing 200-250 g. Dosage: 10 mg/kg/day. Administration: Orally; six weeks. Result: Treatment persistently restored the increased body weight, which was significantly observed at the ninth week until the end of the experimental period.
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• In Vitro:
  Western blot analysis. Cell line: The human melanoma cell line M10, Peripheral blood mononuclear cells, The human Jurkat CD4+ T cell leukemia cell line, the human promyelocytic leukemia cell line HL-60, the epithelial colon cancer HCT116 cells, non adherent mononuclear cells (NAMNC). Concentration: 2.5, 5, 10, 20, 40 μM for Jurkat cells; 20 and 40 μM for HCT116 cells; 40 μM for normal NAMNC, M10 melanoma, HL-60 promyelocytic leukemia, and HT-29 colon cancer cells Incubation time: 2 days for Jurkat cells; 2 or 4 days for HCT116 cells; 2 days for NAMNC, M10 melanoma, HL-60 promyelocytic leukemia, HT-29 colon cancer. Result: Reduced by > 50% the MGMT level at the concentration of 40 μM for Jurkat cells, whereas little or no effect was found when lower concentrations were used. Downregulation of MGMT expression is produced at 40 μM for HCT116 cells. Provoked an ~50% reduction of MGMT level at 40 μM in normal NAMNC, and HL-60 promyelocytic leukemia, HT-29 colon cancer cells except for melanoma M10 cells that showed no downregulation of the protein.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Tetrahydrolipstatin

Quick Database Links

Gene Symbol

Fatty Acid Synthase