货号	规格	价格	上海	北京	珠海	重庆	武汉
S84937-5mg	≥98%	￥990.00 S84937-5mg ￥990.00 3-5天	0 货期：3-5天	-	-	-	-
S84937-10mg	≥98%	￥1560.00 S84937-10mg ￥1560.00 3-5天	0 货期：3-5天	-	-	-	-
S84937-50mg	≥98%	￥4290.00 S84937-50mg ￥4290.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

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

靶点：

NPY Y5 receptor;NeuropeptideYReceptor

体外研究：

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 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

体内研究：

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 in body-weight gain at day 35

参考文献：

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.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.461 ml	12.303 ml	24.606 ml
5 mM	0.492 ml	2.461 ml	4.921 ml
10 mM	0.246 ml	1.23 ml	2.461 ml
50 mM	0.049 ml	0.246 ml	0.492 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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