Cetilistat

- Overview
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    Background
    
    Cetilistat is an inhibitor of pancreatic lipase. It inhibited rat and human pancreatic lipase activity with an IC50 of 54.8 nmol/l, and 5.95 nmol/l, respectively. When cetilistat was orally administered simultaneously with fat emulsion to Sprague-Dawley rats, the elevation in plasma triglyceride concentration by oral fat loading was reduced by cetilistat in a dose-dependent manner at 3, 10, 30, and 100 mg/kg, indicating that cetilistat reduces intestinal fat absorption in rats. Furthermore, cetilistat was administered to DIO F344 rats as food admixture in a high-fat diet at 4.9, 14.9, or 50.7 mg/kg/day for three weeks. Both triglyceride and nonesterified fatty acid content in the feces were dose-dependently and drastically increased, suggesting the intestinal breakdown of fat and excretion. Body weight (BW) gain and white adipose tissue (WAT) weight were also reduced in a dose-dependent manner. Thus cetilistat ameliorates obesity and hyperlipidemia in DIO (diet-induced obesity rats) and useful for the study of human obesity.
    1. Yamada Y, et al. Cetilistat (ATL-962), a novel pancreatic lipase inhibitor, ameliorates body weight gain and improves lipid profiles in rats. Horm Metab Res. 2008 Aug;40(8):539-43.
- Properties
  - Alternative Name
    
    ATL-962; 2-(hexadecyloxy)-6-methyl-4H-benzo[d][1,3]oxazin-4-one
    
    CAS Number
    
    282526-98-1
    
    Molecular Formula
    
    C25H39NO3
    
    Molecular Weight
    
    401.58
    
    Purity
    
    98.00%
    
    Solubility
    
    Insoluble in DMSO; ≥4.12 mg/mL in EtOH (Need ultrasonic and warming); insoluble in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only