PF04620110 是一种口服有效的甘油二酯酰基转移酶 -1(DGAT1)选择性抑制剂,IC50为 19 nM。
产品描述
PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.
体外活性
Ampiroxicam (<150 μM) dose-dependently decreases the proliferation of Panc-1 cells. [1] Ampiroxicam (50 μM) results in decreased expression of Sp1, Sp3, Sp4, and VEGFR1 proteins in Panc-1 cells and L3.6pl cells as determined by Western blot analysis. Ampiroxicam (50 μM) results in increased phosphorylation of MAPK1/2 in Panc-1 cells and L3.6pl cells. [2]
体内活性
In Rats, PF-04620110 reduces plasma triglyceride levels t doses of ≥0.1 mg/kg following a lipid challenge. [1] DGAT1 inhibition by PF-04620110 causes an enrichment of polyunsaturated fatty acids within the TG class of lipids in rodents. [2]
Cas No.
1109276-89-2
分子式
C21H24N4O4
分子量
396.447
别名
PF04620110;PF 04620110
储存和溶解度
DMSO:7.9 mg/mL (20 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years