Anamorelin hydrochloride, 胃泌素受体激动剂

CAS: 861998-00-7 货号: A656178 分子式: C31H43ClN6O3 分子量: 583.16 PubChem CID: 16072155
有货
级别和纯度: 10mM in DMSO
别名
盐酸阿拉莫林
储存条件
干燥,-80℃储存
运输条件
特低温运输
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规格
库存
价格
数量
1ml
A656178-1ml
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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述

AnaMorelin hydrochloride (RC-1291 hydrochloride) 是生长素受体激动剂,根据 FLIPR 检测,得到 EC50=0.74 nM。

Anamorelin (RC-1291) hydrochloride is a potent ghrelin receptor agonist with EC 50 value of 0.74 nM in the FLIPR assay.

In Vitro

In the FLIPR assay, Anamorelin (ANAM) shows significant agonist activity on the ghrelin receptor, with EC 50 value of 0.74 nM. No significant antagonist activity is observed with Anamorelin at concentrations of up to 1,000 nM. In the binding experiments, Anamorelin binds to the ghrelin receptor with a binding affinity constant (K i ) of 0.70 nM. In the competition assay with radiolabeled ibutamoren ( 35 S-MK-677; another ghrelin receptor agonist) Anamorelin (ANAM) is also found to bind with high affinity to the ghrelin receptor (IC 50 =0.69 nM). In rat pituitary cells incubated with Anamorelin, there is a dose-dependent stimulatory effect on GH release and the potency (EC 50 ) is 1.5 nM. Anamorelin is screened for activity against a set of over 100 receptors, ion channels, transporters, and enzymes. Anamorelin demonstrates binding to the tachykinin neurokinin 2 (NK 2 ) site (IC 50 =0.021 μM); however, a subsequent NK 2 functional assay demonstrates no functional activity. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In rats, Anamorelin (ANAM) at an oral dose of 3, 10, or 30 mg/kg once daily significantly increases both food intake and body weight from Day 2 to Day 7 of treatment compared with the vehicle control. The cumulative change in food intake and weight gain increases dose-dependently, and these changes are significant at all dose levels (P<0.05) compared to the control. Administration of Anamorelin at a single oral dose of 3, 10, or 30 mg/kg induces a dose-dependent increase in plasma GH levels and GH AUC 0-6h in rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:Ki: 0.7 nM (ghrelin receptor), EC50: 0.74 nM (ghrelin receptor)

规格

别名
盐酸阿拉莫林
规格或纯度
10mM in DMSO
英文名称
Anamorelin hydrochloride
生化机理
Anamorelin (RC-1291) 盐酸盐是一种强效胃泌素受体激动剂,在 FLIPR 试验中的 EC 50 值为 0.74 nM。
储存条件
干燥,-80℃储存
运输条件
特低温运输
作用类型
激动剂
作用机制
胃泌素受体激动剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CC(C)(C(=O)N[C@H](CC1=CNC2=CC=CC=C21)C(=O)N3CCC[C@](C3)(CC4=CC=CC=C4)C(=O)N(C)N(C)C)N.Cl
关联CAS
PubChem CID
分子量
583.16

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批号(Lot Number) 证书类型 货号
J2613192 分析证书 A656178
溶液计算器