Cas No.: | 328232-95-7 |
Chemical Name: | N-[1-(2-fluorophenyl)pyrazol-3-yl]-1'-oxospiro[cyclohexane-4,3'-furo[3,4-c]pyridine]-1-carboxamide; |
Synonyms: | MK0557,MK 0557 |
SMILES: | O=C([C@H]1CC[C@@](C2=C3C=CN=C2)(OC3=O)CC1)NC4=NN(C5=CC=CC=C5F)C=C4 |
Formula: | C22H19FN4O3 |
M.Wt: | 406.41 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Publication: | [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 clinica |
Description: | MK-0557 is a highly selective, orally available neuropeptide Y5 receptor antagonist with a Ki of 1.6 nM. |
In Vitro: | 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]. |