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  • SNT-207707
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SNT-207707

SNT-207707是一种有效,选择性,有口服活性的黑素皮质素受体(melanocortinMC-4)拮抗剂,IC50值为8nM(结合)和5nM(功能)。

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  • 货号: ajcx12620
  • CAS: 1064662-40-3
  • 别名:
  • 分子式: C32H44ClN5O
  • 分子量: 550.18
  • 纯度: >98%
  • 溶解度: DMSO: ≥ 250 mg/mL (454.40 mM); Methanol: 250 mg/mL (454.40 mM)
  • 储存: Store at -20°C
  • 库存: 现货

Background

SNT-207707 is a selective, potent and orally active melanocortin MC-4 receptor antagonist with an IC50 of 8 nM (binding) and 5 nM (function) on the MC-4 receptor.


SNT-207707 binds to the MC-4 receptor with an affinity of 8 nM and shows a more than 200-fold selectivity vs. MC-3 and MC-5. SNT207858 is a 22 nM MC-4 antagonist with a 170-fold selectivity vs. MC-3 and a 40-fold selectivity versus MC-5[1].


Single subcutaneous injection of 20 mg/kg of SNT-207707 distinctly increases food intake of the mice. Once daily oral administration of both compounds SNT207858 and SNT-207707 starting the day after tumor implantation significantly reduces the tumor induced weight loss[1].


[1]. Weyermann P, et al. Orally available selective melanocortin-4 receptor antagonists stimulate food intake and reduce cancer-induced cachexia in mice. PLoS One. 2009;4(3):e4774.

Protocol

Animal experiment:

Mice[1]Twelve weeks old male CD-1 mice are dosed by gavage with either SNT-207707 or SNT207858 at 60 mg/kg (n=9 per compound). At 1, 3, and 6 hrs post-dose, 3 mice from each compound group are euthanized with CO2. Blood is collected by cardiac puncture, plasma is isolated immediately and then kept on dry ice until analysis[1].

参考文献:

[1]. Weyermann P, et al. Orally available selective melanocortin-4 receptor antagonists stimulate food intake and reduce cancer-induced cachexia in mice. PLoS One. 2009;4(3):e4774.

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