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.
CA3 has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties.
YM 511 is a potent aromatase (CYP19) inhibitor.
|YM 298198 hydrochloride
YM 298198 hydrochloride is a highly potent, selective non-competitive mGlu 1 antagonist.
YM 022 is a highly potent, selective non-peptide CCK 2 antagonist.
YK 3-237 is a sIRT1 activator.
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