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.
|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.|
|Incubation time||4 h|
|Animal models||Wistar rats|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||10 mM in DMSO|
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.
ML-281 is a potent ans selective STK33 inhibitor with IC50 value of 14 nM.
ML-265 (TEPP-46) is a potent and selective activator of recombinant pyruvate kinase M2 (PKM2).
LB-100 is a water soluble protein phosphatase 2A (PP2A) inhibitor, with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells.
Compstatinis is a 13-residue cyclic peptide, binds to complement component C3 and inhibits complement activation with IC50 of 12 μM.
Azaserine is an inhibitor of the rate limiting step of the hexosamine biosynthethic pathway (HBP) and an irreversible inhibitor of GGT1 (gamma-Glutamyltranspeptidase).
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.