中文名称: | 阿拉莫林 | ||||
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英文名称: | Anamorelin | ||||
别名: | 阿拉莫林 2-amino-N-((R)-1-((R)-3-benzyl-3-(1,2,2-trimethylhydrazinecarbonyl)piperidin-1-yl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-2-methylpropanamide | ||||
CAS No: | 249921-19-5 | 分子式: | C31H42N6O3 | 分子量: | 546.7 |
CAS No: | 249921-19-5 | ||||
分子式: | C31H42N6O3 | ||||
分子量: | 546.7 |
基本信息
产品编号: |
A10105 |
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产品名称: |
Anamorelin |
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CAS: |
249921-19-5 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
6个月 |
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分子量: |
546.70 |
-20℃ |
1个月 |
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化学名: |
2-amino-N-((R)-1-((R)-3-benzyl-3-(1,2,2-trimethylhydrazinecarbonyl)piperidin-1-yl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-2-methylpropanamide |
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Solubility (25°C): |
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体外:
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DMSO |
100mg/mL (182.91mM) |
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Ethanol |
79mg/mL (144.5mM) |
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Water |
Insoluble |
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体内(现配现用): |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
1.8292mL |
9.1458mL |
18.2916mL |
5mM |
0.3658mL |
1.8292mL |
3.6583mL |
10mM |
0.1829mL |
0.9146mL |
1.8292mL |
50mM |
0.0366mL |
0.1829mL |
0.3658mL |
生物活性
产品描述 |
一种具有口服活性的、高亲和力的ghrelin receptor选择性激动剂。 |
靶点 |
ghrelin receptor |
0.74nM(EC50) |
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体外研究 |
In the FLIPR assay,Anamorelin (ANAM) shows significant agonist activity on the ghrelin receptor,with EC50 value of 0.74nM.No significant antagonist activity is observed with Anamorelin at concentrations of up to 1,000nM.In the binding experiments,Anamorelin binds to the ghrelin receptor with a binding affinity constant (Ki) of 0.70nM.In the competition assay with radiolabeled ibutamoren (35S-MK-677;another ghrelin receptor agonist) Anamorelin (ANAM) is also found to bind with high affinity to the ghrelin receptor (IC50=0.69nM).In rat pituitary cells incubated with Anamorelin,there is a dosedependent stimulatory effect on GH release and the potency (EC50) is 1.5nM.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 (NK2) site (IC50=0.021μM);however,a subsequent NK2 functional assay demonstrates no functional activity. |
体内研究 |
In rats,Anamorelin (ANAM) at an oral dose of 3,10,or 30mg/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 30mg/kg induces a dose-dependent increase in plasma GH levels and GH AUC0-6h in rats. |
推荐实验方法(仅供参考)
激酶实验: |
For the competition assay,Anamorelin (ANAM) concentrations (1 pM-10μM) are added to the membranes together with 35SMK-677.Nonspecific binding is determined by adding 10μM nonlabeled MK-677.The mixture is incubated at 30℃ for 60 min,followed by application of the samples to GF/B filters,which has been pretreated with 0.5 % PEI for 60 min.The filters are subsequently washed in 0.9 % NaCl and counted using an OptiPhase counter. |
动物实验: |
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Rats For the assessment of food intake and body weight,rats are divided into four groups:Anamorelin 3mg/kg (n=7),10mg/kg (n=7),or 30mg/kg (n=7),or vehicle control (n=8),and 100μL blood samples are collected before and 0.25,0.5,1,2,3,4,5,and 6h after single dosing.Rats are anesthetized with sodium pentobarbital 64.8mg/kg.A catheter filled with heparinized saline solution is inserted in the left femoral artery for blood collection and fitted with an extension tube,1mL sampling syringe,and a three-way cock to allow excess blood to return.Plasma levels of GH are measured immunochemically using a Rat Growth Hormone EIA kit and microplate reader.Measurements are performed in duplicate.Area under the GH concentration curve from 0 to 6h (AUC0-6h) postdose and the time course of GH plasma concentrations are evaluated. Pig In pigs (n=6 per group),Anamorelin is dosed directly into the gastric lumen via the dosing catheter.Blood samples are collected for the stimulation profile of GH at 30 and 15 min before,and 0,5,15,30,45,60,and 120 min following dosing.Animals received either a single dose (3.5mg/kg),or once-daily administration (1mg/kg) for 7 days and stimulation profiles are taken after the first and seventh dose of Anamorelin.To assess IGF-1 levels,pigs receive either placebo or Anamorelin for 7 days (1mg/kg/day),and the following 7 days the two treatments are crossed over.A single blood sample is taken once a day immediately before dosing. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )