PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.
PF-04620110 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Bone marrow-derived macrophages (BMDMs)
50 µM
2 hours
Suppressed fatty acid-induced NLRP3 inflammasome activation, reduced secretion of IL-1β and IL-18, but did not affect TNF-α secretion.
Diabetes Metab J. 2019 Oct;43(5):683-699.
HT-29 cells
8 nM
To evaluate the inhibitory effect of PF-04620110 on triglyceride synthesis in HT-29 cells, showing an IC50 of 8 nM.
ACS Med Chem Lett. 2011 Mar 18;2(5):407-12.
PF-04620110 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Sprague-Dawley rats
Acute lipid challenge model
Oral
0.1, 1, or 10 mg/kg
Single dose
To assess the effect of PF-04620110 on plasma triglyceride levels in an acute lipid challenge model, showing significant reduction in plasma triglyceride levels at 2 hours post-dose.
ACS Med Chem Lett. 2011 Mar 18;2(5):407-12.
C57BL/6 mice
High-fat diet (HFD)-induced diabetic Mice model
Oral
3 mg/kg
Once daily for 4 weeks
Reduced HFD-induced plasma levels of IL-1β and IL-18, and decreased fasting and basal blood glucose levels.
United States, California
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Pfizer Investigational Site
Chula Vista, California, United States, 91911
United States, Florida
Pfizer Investigational Site
DeLand, Florida, United States, 32720
Pfizer Investigational Site
Miami Gardens, Florida, United States, 33169 收起 <<
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