| Description | PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM. |
| In vitro | 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] |
| In vivo | 在大鼠中，PF-04620110在≥0.1 mg/kg的剂量下，随后的脂质挑战测试中能够降低血浆甘油三酯水平。[1] 通过抑制DGAT1，PF-04620110导致啮齿动物体内TG类脂质中多不饱和脂肪酸的含量增加。[2] |
| Target activity | DGAT-1:19 nM |
| Synonyms | PF04620110, PF 04620110 |
| molecular weight | 396.44 |
| Molecular formula | C21H24N4O4 |
| CAS | 1109276-89-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 7.9 mg/mL (20 mM) |
| References | 1. Dow RL, et al. ACS Med Chem Lett. 2011, 2(5), 407-412. 2. Maciejewski BS, et al. Am J Physiol Gastrointest Liver Physiol. 2013, 304(11), G958-969. |