PF-04620110,1109276-89-2

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PF-04620110

CAS No. : 1109276-89-2

MCE 国际站：PF-04620110

产品活性：PF-04620110 是一种有效、选择性的，有口服活性的甘油二酯酰基转移酶 -1 (DGAT1) 抑制剂，IC₅₀ 值为 19 nM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Acyltransferase

In Vitro: 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).

In Vivo: 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.

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