Anamorelin

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Chemical Structure| 249921-19-5 同义名 : RC-1291; ONO-7643; ST-1291
CAS号 : 249921-19-5
货号 : A424450
分子式 : C31H42N6O3
纯度 : 98+%
分子量 : 546.7
MDL号 : MFCD11973671
存储条件：

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(192.06 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Anamorelin is an orally active GHS-R (ghrelin receptor) agonist in development for non-small cell lung cancer (NSCLC)-related anorexia/cachexia. Anamorelin exhibited both orexigenic and anabolic properties via ghrelin mimetic activity and transient increases in growth hormone, but does not promote tumor growth like GH and insulin-like growth factor-1. ANAM showed significant agonist activity on the ghrelin receptor with EC50 value of 0.74nM in a FLIPR assay and stimulated GH release with EC50 value of 1.5nM in rat pituitary cells. Administration of Anamorelin orally at dose of 3, 10, or 30 mg/kg once daily significantly increased both food intake and body weight from day 2 to day 7 in rats. A single oral dose of 3, 10, or 30 mg/kg Anamorelin induced a dose-dependent increase in plasma GH levels and GH AUC0-6h in rats.
作用机制 Anamorelin works through ghrelin mimetic activity.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.83mL

0.37mL

0.18mL

9.15mL

1.83mL

0.91mL

18.29mL

3.66mL

1.83mL
参考文献

[1]Northrup R, Kuroda K, et al. Effect of ghrelin and anamorelin (ONO-7643), a selective ghrelin receptor agonist, on tumor growth in a lung cancer mouse xenograft model. Support Care Cancer. 2013 Sep;21(9):2409-15.

[2]Pietra C, Takeda Y, et al. Anamorelin HCl (ONO-7643), a novel ghrelin receptor agonist, for the treatment of cancer anorexia-cachexia syndrome: preclinical profile. J Cachexia Sarcopenia Muscle. 2014 Dec;5(4):329-37.