货号:A424450
同义名:
RC-1291; ONO-7643
Anamorelin is a ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay.
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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] |
Dose | Nude Mice: 2 mg/kg[1] (i.p.) Rat: 3 mg/kg - 30 mg/kg[2] (p.o.) |
Administration | i.p., p.o. |
计算器 | ||||
存储液制备 | ![]() |
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 |
CAS号 | 249921-19-5 |
分子式 | C31H42N6O3 |
分子量 | 546.7 |
SMILES Code | [H][C@](CC1=CNC2=CC=CC=C21)(NC(C(C)(C)N)=O)C(N3CCC[C@@](C(N(C)N(C)C)=O)(CC4=CC=CC=C4)C3)=O |
MDL No. | MFCD11973671 |
别名 | RC-1291; ONO-7643; ST-1291 |
运输 | 蓝冰 |
InChI Key | VQPFSIRUEPQQPP-MXBOTTGLSA-N |
Pubchem ID | 9828911 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C |
溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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