328232-95-7

• 常用中文名：MK-0557
• 常用英文名：MK 0557
• CAS号：328232-95-7
• 分子式：C₂₂H₁₉FN₄O₃
• 分子量：406.41000
• 相关类别： 信号通路 G 蛋白偶联受体/G 蛋白 神经肽Y受体
• 发布时间：2016-03-25 20:12:15
• 更新时间：2024-01-11 18:40:41
• 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。

名称

• 中文名: MK-0557
• 英文名: N-[1-(2-fluorophenyl)pyrazol-3-yl]-1'-oxospiro[cyclohexane-4,3'-furo[3,4-c]pyridine]-1-carboxamide
• 英文别名: UNII-HVE36P8422; MK-0557; 1'-cyclohexane]-4'-carboxamide; MK 0557

物化性质

• 分子式: C₂₂H₁₉FN₄O₃
• 分子量: 406.41000
• 精确质量: 406.14400
• PSA: 89.34000
• LogP: 3.02290
• 储存条件: 2-8℃

生物活性

• 描述: MK-0557是具有高度选择性,口服活性的神经肽Y5受体拮抗剂,Ki值为1.6 nM。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 神经肽Y受体
  研究领域 >> 代谢疾病
• 靶点:

  Ki: 1.6 nM (Y5)[1]

• 体外研究: MK-0557拮抗NPY5R选择性激动剂对C57BL/6J小鼠的体重增加和饮食过多的影响,并显着抑制饮食诱导的肥胖(DIO)小鼠的体重增加。当正常食物中的瘦小鼠转换为中等高脂肪饮食(4.2千卡/克)并用30毫克/千克PO QD的MK-0557治疗时,MK-0557导致第35天体重增加减少40％ [2]。
• 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.

合成路线

569351-62-8 ~% 328232-95-7

文献：Iida, Takehiko; Satoh, Hiroki; Maeda, Kenji; Yamamoto, Yuhei; Asakawa, Ken-Ichi; Sawada, Naotaka; Wada, Toshihiro; Kadowaki, Chie; Itoh, Takahiro; Mase, Toshiaki; Weissman, Steven A.; Tschaen, Dave; Krska, Shane; Volante Journal of Organic Chemistry, 2005 , vol. 70, # 23 p. 9222 - 9229

870466-68-5 ~% 328232-95-7

文献：Iida, Takehiko; Satoh, Hiroki; Maeda, Kenji; Yamamoto, Yuhei; Asakawa, Ken-Ichi; Sawada, Naotaka; Wada, Toshihiro; Kadowaki, Chie; Itoh, Takahiro; Mase, Toshiaki; Weissman, Steven A.; Tschaen, Dave; Krska, Shane; Volante Journal of Organic Chemistry, 2005 , vol. 70, # 23 p. 9222 - 9229

3034-31-9 ~% 328232-95-7

文献：Iida, Takehiko; Satoh, Hiroki; Maeda, Kenji; Yamamoto, Yuhei; Asakawa, Ken-Ichi; Sawada, Naotaka; Wada, Toshihiro; Kadowaki, Chie; Itoh, Takahiro; Mase, Toshiaki; Weissman, Steven A.; Tschaen, Dave; Krska, Shane; Volante Journal of Organic Chemistry, 2005 , vol. 70, # 23 p. 9222 - 9229

17159-79-4 ~% 328232-95-7

文献：Iida, Takehiko; Satoh, Hiroki; Maeda, Kenji; Yamamoto, Yuhei; Asakawa, Ken-Ichi; Sawada, Naotaka; Wada, Toshihiro; Kadowaki, Chie; Itoh, Takahiro; Mase, Toshiaki; Weissman, Steven A.; Tschaen, Dave; Krska, Shane; Volante Journal of Organic Chemistry, 2005 , vol. 70, # 23 p. 9222 - 9229

923984-29-6 ~% 328232-95-7

文献：MERCK and CO., INC.; BANYU PHARMACEUTICAL CO., LTD. Patent: WO2007/16028 A2, 2007 ; Location in patent: Page/Page column 13; 14 ; WO 2007/016028 A2

685094-07-9 328233-23-4 ~17% 328232-95-7

文献：Haga, Yuji; Sakamoto, Toshihiro; Shibata, Takunobu; Nonoshita, Katsumasa; Ishikawa, Makoto; Suga, Takuya; Takahashi, Hirobumi; Takahashi, Toshiyuki; Takahashi, Hidekazu; Ando, Makoto; Murai, Takashi; Gomori, Akira; Oda, Zenjun; Kitazawa, Hidefumi; Mitobe, Yuko; Kanesaka, Maki; Ohe, Tomoyuki; Iwaasa, Hisashi; Ishii, Yasuyuki; Ishihara, Akane; Kanatani, Akio; Fukami, Takehiro Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 19 p. 6971 - 6982

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