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Cetilistat

SKU: orb1225440

Description

Cetilistat is an inhibitor of pancreatic and gastrointestinal lipases. It has great treatment of obesity in both diabetic and non-diabetic patients.

Research Area

Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number282526-98-1
MW401.58
Purity>98% (HPLC)
FormulaC25H39NO3
SMILESO=C1C2=CC(C)=CC=C2N=C(OCCCCCCCCCCCCCCCC)O1
TargetOthers
SolubilitySoluble in DMSO, chloroform

Bioactivity

In Vivo
Cetilistat (3, 10, 30, or 100 mg/kg) reduces intestinal fat absorption by inhibiting pancreatic lipase activity in male SD rats. 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. Animal model: Fifty male SD rats (eight weeks of age). Dosage: 3, 10, 30, or 100 mg/kg. Administration: Orally administered; prepared in 0.5 % methylcellulose (MC) suspension. Result: Dose-dependently reduced AUC 0-6 h of plasma triglyceride induced by oral loading of Intrafat 20%. The effect was statistically significant at 3 mg/kg, reaching 45% reduction, while an almost 90 % reduction was achieved at 100 mg/kg. Animal model: Male diet-induced obesity (DIO) F344 rats (five weeks of age). Dosage: 4.9, 14.9, or 50.7 mg/kg. Administration: Administered as food admixture in a high-fat diet; once a day; for three weeks. Result: Significantly and dose-dependently reduced body weight gain compared with control.
In Vitro
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.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

ATL-962 | ATL962 | ATL 962 | Cetilistat

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Protocol Information

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500 mg
100 mg
$ 80.00
200 mg
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