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.
Wilforine is a sesquiterpene pyridine alkaloid; important bioactive compound in T. wilfordii plants, and is effective in treating idiopathic pulmonary fibrosis.
Wilfortrine is an immunomodulatory compound isolated from Tripterygium wilfordii.
Etanercept is a dimeric fusion protein consisting of two ligand-binding domains of human p75 tumor necrosis factor receptor and the human IgG1 Fc portion.
Tocilizumab is a humanized monoclonal antibody that binds to the interleukin-6 receptor, MW: 148 KD.
Lambrolizumabis a potent, highly selective, fully humanized immunoglobulin (Ig) G4-kappa monoclonal antibody against PD-1 with potential immune checkpoint inhibitory and antineoplastic activities. MW : 146.286 KD.
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