Cetilistat（CAS：282526-98-1）

Cetilistat (CAS Registry Number: 282526-98-1) is a novel selective gastrointestinal lipase inhibitor, with the chemical name 2-(Hexadecyloxy)-6-methyl-4H-3,1-benzoxazin-4-one. Its molecular formula is C₂₅H₃₉NO₃, and the molecular weight is 401.58.

Physicochemical Properties

Cetilistat appears as a white to off-white crystalline powder, with a melting point of 74~76℃. It is almost insoluble in water, while soluble in organic solvents including methanol, ethanol, dichloromethane and acetone. The compound maintains stable properties under conventional storage conditions (cool, dry, sealed and away from light), with good tolerance to light and heat.

Mechanism of Action and Pharmacological Properties

Cetilistat is a long-acting, reversible gastrointestinal lipase inhibitor. It exerts its pharmacological effect by specifically forming a covalent bond with the active serine site of gastric and pancreatic lipases, thus inactivating the enzymes. This effect blocks the hydrolysis and intestinal absorption of dietary triglycerides, reduces the body's caloric intake, and achieves the effect of weight control.

After oral administration, cetilistat is hardly absorbed by the gastrointestinal tract with no systemic exposure. It does not act on the central nervous system and has no addiction potential. Compared with similar weight management products, cetilistat has milder gastrointestinal adverse reactions and a wider safety window. The compound is mainly metabolized in the intestinal tract, and the vast majority of the prototype drug and its metabolites are excreted via feces.

Core Application

Cetilistat is mainly used for weight loss and weight maintenance in patients with obesity, and also applicable for weight management in overweight patients with obesity-related complications such as hypertension, hyperlipidemia and type 2 diabetes mellitus.