Chemical Property of Cetilistat
Chemical Property:
- Appearance/Colour:Off-white cryst.
- Vapor Pressure:0mmHg at 25°C
- Melting Point:72.0 to 76.0 °C
- Refractive Index:1.521
- Boiling Point:509.671 °C at 760 mmHg
- PKA:2.96±0.20(Predicted)
- Flash Point:158.925 °C
- PSA：52.33000
- Density:1.027 g/cm3
- LogP:7.35650
- Storage Temp.:2-8°C
- Solubility.:Chloroform (Slightly), Ethyl Acetate (Slightly)
- XLogP3:9.8
- Hydrogen Bond Donor Count:0
- Hydrogen Bond Acceptor Count:4
- Rotatable Bond Count:16
- Exact Mass:401.29299411
- Heavy Atom Count:29
- Complexity:477
- Purity/Quality:
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99%+ *data from raw suppliers
Cetilistat *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:CCCCCCCCCCCCCCCCOC1=NC2=C(C=C(C=C2)C)C(=O)O1
- Recent ClinicalTrials:Study of the Blood Levels and Effects of ATL-962 on Fat Excretion in Obese Subjects
- Recent EU Clinical Trials:A Phase II Multicentre, Double Blind, Placebo Controlled, Parallel Group, Dose Ranging Study of ATL 962 to Assess Weight Loss, Safety and Tolerability in Obese Patients with Type II Diabetes being treated with Metformin, in comparison with orlistat
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Description
Cetilistat (also known as ATL-962) was approved in September 2013 by the Japanese Ministry of Health, Labor and Welfare for the treatment of obesity, limited to patients with both type 2 diabetes mellitus (T2DM) and dyslipidemia, and with a body mass index (BMI)25 kg/m2 in spite of dietary treatment and/or exercise therapy. As with orlistat, cetilistat works via inhibition of pancreatic lipases in the gut to inhibit fat absorption and thereby reduce caloric uptake from diet. The medicinal chemistry program has not been described in the scientific literature, but the patent describing cetilistat also describes the synthesis of analogs with varied aryl substituents and lipophilic tails. The synthesis of cetilistat involves condensation of a hexadecylcarbonochloridate with 2-amino-5-methylbenzoic acid; other analogs were synthesized by varying the carbonochloridate and 2-aminobenzoic acid components. Cetilistat is a potent inhibitor of human and rat pancreatic lipase with IC50s of 15 and 136 nM, respectively, with little inhibition of trypsin or chymotrypsin.
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Uses
A novel pancreatic lipase inhibitor for the treatment of obesity in both diabetic and non-diabetic patients.
