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编 号:F038080
分子式:C21H24N4O4
分子量:396.44
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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100mg
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生物活性:
PF-04620110 is a potent, selective and orally bioavailable diglyceride acyltransferase-1 (DGAT-1) inhibitor with an IC50 of 19 nM.

体内研究:
PF-04620110 (0.1-10 mg/kg; p.o.) reduces plasma triglyceride levels at doses of ≥0.1 mg/kg following a lipid challenge in rat.Animal Model:Sprague?Dawley rats
Dosage:0.1 mg/kg, 1 mg/kg, 10 mg/kg
Administration:Oral administration
Result:Produced a statistically significant reduction in plasma triglyceride excursion at 2 hours to near prelipid load levels.

体外研究:
PF-04620110 is orally bioavailable, has passive permeability(1x10-6 cm/s).PF-04620110 inhibits DGAT-1 with an IC50 of 19 nM, and inhibits triglyceride synthesis with an IC50 of 8 nM in HT-29 cells.PF-04620110 is a highly selective inhibitor of DGAT-1 with >100-fold selectivity against a panel of lipid processing enzymes (human DGAT-2, several human acyl-CoA: cholesterol acyltransferase-1, wax alcohol acyltransferase-1/-2 and monacylglycerol acyltransferase-2/-3, and mouse MGAT-1).
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