PF-04620110 - CAS 1109276-89-2
Catalog number: 1109276-89-2
Category: Inhibitor
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PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.
PF-04620110; PF 04620110; PF04620110. PF-4620110; PF 4620110; PF4620110.
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1.Model-based pharmacokinetic and pharmacodynamic analysis for acute effects of a small molecule inhibitor of diacylglycerol acyltransferase-1 in the TallyHo/JngJ polygenic mouse.
Chae YJ;Song JS;Ahn JH;Bae MA;Lee KR Xenobiotica. 2018 Sep 5:1-10. doi: 10.1080/00498254.2018.1496303. [Epub ahead of print]
The purpose of this study was to evaluate the acute effect of a small molecule inhibitor of DGAT-1 on triglycerides (TG) and cholesterol in polygenic type 2 diabetic TallyHo/JngJ (TH) mice. PF-04620110, a potent and selective DGAT-1 inhibitor, was used as a model compound in this study and which was administered to TH and ICR mice. The concentration of the model compound that produced 50% of maximum lowering of TG level (IC;50;) in TH mice was not significantly different from that in ICR mice, when estimated using the model-based pharmacokinetic and pharmacodynamic assay, a two-compartmental model and an indirect response model. The clearance of the inhibitor in TH mice was fivefold higher than that in ICR mice, suggesting significantly altered pharmacokinetics. Moreover, the in vitro metabolic elimination kinetic parameters (k;e,met;), determined using liver microsomes from TH and ICR mice were 1.24 ± 0.14 and 0.174 ± 0.116 min;-1;, respectively. Thus, we report that the differences in the acute effects of the small molecule DAGT-1 inhibitor between TH mice and ICR mice can be attributed to altered pharmacokinetics caused by an altered metabolic rate for the compound in TH mice.
2.American Chemical Society-239th national meeting--Investigating new therapeutic candidates: part 1. 21-25 March 2010, San Francisco, CA, USA.
Macauley D IDrugs. 2010 May;13(5):289-91.
The American Chemical Society 239th National Meeting, held in San Francisco, included topics covering developments related to the chemical optimization of therapeutics. This conference report highlights selected presentations on agents under investigation for the treatment of neurological disorders, malaria, HBV and diabetes. Investigational drugs discussed include PF-4888086, PF-4778574 and SAM-531 (all Pfizer Inc), a series of spirotetrahydro-beta-carbolines from Novartis AG, a series of biaryl ether analogs from Merck & Co Inc, and PF-04620110 (Pfizer Inc/Bristol-Myers Squibb Co).
3.Pharmacological inhibition of diacylglycerol acyltransferase-1 and insights into postprandial gut peptide secretion.
Maciejewski BS;Manion TB;Steppan CM World J Gastrointest Pathophysiol. 2017 Nov 15;8(4):161-175. doi: 10.4291/wjgp.v8.i4.161.
AIM: ;To examine the role that enzyme Acyl-CoA:diacylglycerol acyltransferase-1 (DGAT1) plays in postprandial gut peptide secretion and signaling.;METHODS: ;The standard experimental paradigm utilized to evaluate the incretin response was a lipid challenge. Following a lipid challenge, plasma was collected ;via; cardiac puncture at each time point from a cohort of 5-8 mice per group from baseline at time zero to 10 h. Incretin hormones [glucagon like peptide-1 (GLP-1), peptide tyrosine-tyrosine (PYY) and glucose dependent insulinotropic polypeptide (GIP)] were then quantitated. The impact of pharmacological inhibition of DGAT1 on the incretin effect was evaluated in WT mice. Additionally, a comparison of loss of DGAT1 function either by genetic ablation or pharmacological inhibition. To further elucidate the pathways and mechanisms involved in the incretin response to DGAT1 inhibition, other interventions [inhibitors of dipeptidyl peptidase-IV (sitagliptin), pancreatic lipase (Orlistat), GPR119 knockout mice] were evaluated.;RESULTS: ;DGAT1 deficient mice and wildtype C57/BL6J mice were lipid challenged and levels of both active and total GLP-1 in the plasma were increased. This response was further augmented with DGAT1 inhibitor PF-04620110 treated wildtype mice.
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CAS 1109276-89-2 PF-04620110

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