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Cetilistat Lipase inhibitor

Cat.No.S4930

Cetilistat (ATL962) is a novel highly lipophilic benzoxazinone that inhibits gastrointestinal and pancreatic lipases. It shows a good safety and tolerability profile in vivo
Cetilistat Lipase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 401.58

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S493001 Ethanol]8 mg/mL]false]DMSO]3 mg/mL]false]Water]Insoluble]false Purity: 98.99%
98.99

Chemical Information, Storage & Stability

Molecular Weight 401.58 Formula

C25H39NO3

 Storage (From the date of receipt)
CAS No. 282526-98-1 -- Storage of Stock Solutions

Synonyms ATL962 Smiles CCCCCCCCCCCCCCCCOC1=NC2=C(C=C(C=C2)C)C(=O)O1

Solubility

In vitro
Batch:

Ethanol : 8 mg/mL

DMSO : 3 mg/mL (7.47 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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%
% Tween 80
% ddH2O
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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
human pancreatic lipase [1]
5.95 nM
rat pancreatic lipase [1]
54.8 nM
In vitro
Cetilistat inhibits rat and human pancreatic lipase activity with an IC50 of 54.8 nM and 5.95 nM, respectively[1].
In vivo
Cetilistat reduces intestinal fat absorption in rats and decreases energy intake without CNS side effects. This compound ameliorates obesity and hyperlipidemia in DIO rats, a plausible animal model of the most common type of human obesity[1].
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00148382 Completed
Obesity
Alizyme
 April 2005 Phase 1

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