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MK-0557

CAS No. : 328232-95-7

MCE 国际站：MK-0557

产品活性：MK-0557是具有高度选择性，口服活性的神经肽Y5受体拮抗剂，K_i值为1.6 nM。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Neuropeptide Y Receptor

In Vitro: Neuropeptide Y (NPY) is a potent orexigenic neuropeptide, and antagonism of NPY Y1 and NPY Y5 receptors (NPYxR) is considered a potentially important anti-obesity drug target. MK-0557 has a K_i=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.

In Vivo: 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.

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