MK 0557

MK-0557 is a highly selective, orally available neuropeptide Y5 receptor antagonist with a Ki of 1.6 nM.

Signaling Pathways >> GPCR/G Protein >> Neuropeptide Y Receptor

Research Areas >> Metabolic Disease

Ki: 1.6 nM (Y5)[1]

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. 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, MK-0557 causes a 40% reduction inbody-weight gain at day 35[2].

[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.

Velneperit | HT-2157 | BIIE 0246 | Galanin (1-16) (mouse, porcine, rat) | JNJ-31020028 | CGP 71683 HCl | FR252384 | Galanin (human) acetate salt | Galanin (1-13)-Substance P (5-11) amide | Galanin (1-13)-Pro-Pro-(Ala-Leu-)₂Ala amide | Neuropeptide Y (13-36) (human, rat) trifluoroacetate salt | Neuropeptide Y(29-64) | Pancreatic Polypeptide, bovine | Pancreatic Polypeptide (human) trifluoroacetate salt