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Cetilistat

Cat. No. M6192
Cetilistat Structure
Synonym:

ATL-962

Size Price Availability Quantity
200mg USD 80 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Cetilistat is highly lipophilic, which facilitated their dissolution in the GTL without the need of a vehicle. Although cetilistat is a benzoxazinone lipase inhibitor, orlistat reacts with the nucleophilic serine of lipases via its β-lactone moiety, resulting in a covalent complex.

Protocol
Cell Experiment
Cell lines acinar cells
Preparation method Pancreatic acini were harvested and preincubated with 50 μmol/L orlistat or cetilistat, after which linoleic acid (LA) or GTL was added, followed by incubation for 4 hours.
Concentrations 50 μmol/L
Incubation time 4 h
Animal Experiment
Animal models Wistar rats
Formulation GTL
Dosages 25 mg/mL
Administration i.v.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 401.58
Formula C25H39NO3
CAS Number 282526-98-1
Purity >98%
Solubility 10 mM in DMSO
Storage at -20°C
References

Computational analysis and enzyme assay of inhibitor response to disease single nucleotide polymorphisms (SNPs) in lipoprotein lipase.
He D, et al. J Bioinform Comput Biol. 2016 Oct;14(5):1650028. PMID: 27427383.

Acute lipotoxicity regulates severity of biliary acute pancreatitis without affecting its initiation.
Durgampudi C, et al. Am J Pathol. 2014 Jun;184(6):1773-84. PMID: 24854864.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Cetilistat, ATL-962 supplier, inhibitors

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