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Cetilistat

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Chemical Structure| 282526-98-1 同义名 : ATL-962
CAS号 : 282526-98-1
货号 : A117014
分子式 : C25H39NO3
纯度 : 98%
分子量 : 401.582
MDL号 : MFCD09839697
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 Cetilistat is a novel 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. 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[3]. Cetilistat was well tolerated at all doses examined and tolerability appeared to be improved relative to orlistat. Faecal fat excretion in the cetilistat groups was at least comparable to the orlistat 120 mg t.i.d. group[4]. Treatment with cetilistat 80 or 120 mg t.i.d., or with orlistat 120 mg t.i.d., significantly reduced body weight and improved glycemic control relative to placebo in obese diabetic patients[5]. In phase II clinical trials in obese patients and in obese patients with type 2 diabetes, cetilistat administered for 12 weeks significantly reduced body weight, serum low-density lipoprotein (LDL) cholesterol and total cholesterol in comparison to placebo. Cetilistat showed mild to moderate adverse events, predominantly of gastrointestinal nature (steatorrhea), with an incidence lower than orlistat[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.49mL

0.50mL

0.25mL

12.45mL

2.49mL

1.25mL

24.90mL

4.98mL

2.49mL
参考文献

[1]Andrew Bryson, Stephan de la Motte, et al. Reduction of dietary fat absorption by the novel gastrointestinal lipase inhibitor cetilistat in healthy volunteers.Br J Clin Pharmacol. 2009 Mar; 67(3): 309–315.

[2]Bryson A, de la Motte S, Dunk C. Reduction of dietary fat absorption by the novel gastrointestinal lipase inhibitor cetilistat in healthy volunteers. Br J Clin Pharmacol. 2009 Mar;67(3):309-15.

[3]Yamada Y, Kato T, Ogino H, Ashina S, Kato K. 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

[4]Bryson A, de la Motte S, Dunk C. Reduction of dietary fat absorption by the novel gastrointestinal lipase inhibitor cetilistat in healthy volunteers. Br J Clin Pharmacol. 2009 Mar;67(3):309-15

[5]Kopelman P, Groot Gde H, Rissanen A, Rossner S, Toubro S, Palmer R, Hallam R, Bryson A, Hickling RI. Weight loss, HbA1c reduction, and tolerability of cetilistat in a randomized, placebo-controlled phase 2 trial in obese diabetics: comparison with orlistat (Xenical). Obesity (Silver Spring). 2010 Jan;18(1):108-15

[6]Gras J. Cetilistat for the treatment of obesity. Drugs Today (Barc). 2013 Dec;49(12):755-9