| Bioactivity | Cetilistat (ATL-962), an inhibitor of pancreatic lipase, acts as an effective anti-obesity agent. Cetilistat inhibits rat and human pancreatic lipase activity with IC50s of 54.8 nM, and 5.95 nM, respectively[1]. | ||||||||||||
| Target | IC50: 54.8 nM (rat pancreatic lipase), 5.95 nM (human pancreatic lipase) | ||||||||||||
| Invitro | Cetilistat inhibits rat pancreatic lipase activity with an IC50 of 54.8 nM. Also, Cetilistat inhibits human pancreatic lipase activity with an IC50 of 5.95 nM, which is 9.2 times more potent than for rat pancreatic lipase[1]. | ||||||||||||
| In Vivo | Cetilistat (3, 10, 30, or 100 mg/kg) reduces intestinal fat absorption by inhibiting pancreatic lipase activity in male SD rats[1].Cetilistat (4.9, 14.9, or 50.7 mg/kg; mixed into powdered high-fat diet; once a day; for three weeks) shows anti-obesity and antihyperlipidemic effects on DIO F344 rats by reducing intestinal fat absorption[1]. Animal Model: | ||||||||||||
| Name | Cetilistat | ||||||||||||
| CAS | 282526-98-1 | ||||||||||||
| Formula | C25H39NO3 | ||||||||||||
| Molar Mass | 401.58 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |