| Description | MK-0557 is a selective and orally available antagonist of the neuropeptide Y5 receptor (Ki: 1.6 nM). |
| In vitro | MK-0557在人类NPY5R上的Ki值为1.3 nM，且在黑猩猩、小鼠和大鼠的NPY5R上具有类似的亲和力。在10 μM的浓度下，MK-0557对人类NPY1R、NPY2R、NPY4R或小鼠NPY6R无显著结合活性[2]。 |
| In vivo | MK-0557 在 C57BL/6J 小鼠中，对 NPY5R-selective 激动剂引起的体重增加和暴食行为有拮抗作用，且显著抑制了因饮食引起的肥胖（DIO）小鼠的体重增长。当常规饲料的瘦小鼠转换至中等高脂肪饮食（4.2 kcal/g）并以每日一次口服给予 MK-0557（30 mg/kg PO QD）处理时，到第35天，MK-0557 使体重增长减少了40%[2]。 |
| Target activity | Y5 receptor:1.6 nM (Ki) |
| molecular weight | 406.41 |
| Molecular formula | C22H19FN4O3 |
| CAS | 328232-95-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 25 mg/mL (61.52 mM) |
| References | 1. Fichtner M, et al. Discovery and evaluation of spirocyclic derivatives as antagonists of the neuropeptide Y5 receptor. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2738-43. 2. Erondu N, et al. Neuropeptide Y5 receptor antagonism does not induce clinically meaningful weight loss in overweight and obese adults. Cell Metab. 2006 Oct;4(4):275-82. |