计算溶液所需的质量、体积或浓度。
,适用于对基线干扰要求严格的色谱和分析工作流程。
干燥,-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
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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。
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)
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| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
| 分析证书 | A656178 |