CAS NO: | 328232-95-7 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
生物活性 | MK-0557 is a highly selective, orally available neuropeptideY5receptor antagonist with aKiof 1.6 nM. | ||||||||||||||||
IC50& Target | Ki: 1.6 nM (Y5)[1] | ||||||||||||||||
体外研究 (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 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[2]. | ||||||||||||||||
体内研究 (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 in body-weight gain at day 35[2]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 406.41 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C22H19FN4O3 | ||||||||||||||||
CAS 号 | 328232-95-7 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 200 mg/mL(492.11 mM;Need ultrasonic) H2O :< 0.1 mg/mL(insoluble) 配制储备液
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