MK-0557 是神经肽 Y5 受体的选择性口服拮抗剂，Ki值为1.6 nM。

MK-0557 is a selective and orally available antagonist of the neuropeptide Y5 receptor (Ki: 1.6 nM).

MK-0557 has a Ki=1.3 nM at the human NPY5R, with similar affinities at rhesus, mouse, and rat NPY5R. MK-0557 has no significant binding to the human NPY1R, NPY2R, NPY4R, or mouse NPY6R at concentrations of 10 μM [2].

MK-0557 antagonizes the effects of the NPY5R-selective agonist on body-weight gain and hyperphagia in C57BL/6J mice and significantly suppresses the body-weight gain in diet-induced obese (DIO) mice. MK-0557 causes a 40% reduction in body-weight gain at day 35 when lean mice on regular chow are switched to a medium high-fat diet (4.2 kcal/g) and treated with MK-0557 at 30 mg/kg PO QD[2].

328232-95-7

C22H19FN4O3

406.41

DMSO:25 mg/mL (61.52 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years