(3R)-1-(2-Methylalanyl-D-tryptophyl)-3-(phenylmethyl)-3-piperidinecarboxylic acid 1,2,2-trimethylhydrazide
Anamorelin
CAS: 249921-19-5
Molecular Formula: C31H42N6O3
(3R)-1-(2-Methylalanyl-D-tryptophyl)-3-(phenylmethyl)-3-piperidinecarboxylic acid 1,2,2-trimethylhydrazide - Names and Identifiers
| Name | Anamorelin |
| Synonyms | Rc 1291 ONO-7643 anamorelin Anamorelin Unii-dd5rba1nkf Anamorelin (RC-1291) 3-Piperidinecarboxylic acid, 1-(2-methylalanyl-D-tryptophyl)-3-(phenylmethyl)-, trimethylhydrazide, (3R)- (3R)-1-(2-Methylalanyl-D-tryptophyl)-3-(phenylmethyl)-3-piperidinecarboxylic acid 1,2,2-trimethylhydrazide (R)-1-((S)-2-((1H-indol-3-yl)methyl)-5-amino-5-methyl-4-oxohexanoyl)-3-benzyl-N,N',N'-trimethylpiperidine-3-carbohydrazide 2-amino-N-[(2R)-1-[(3R)-3-benzyl-3-[dimethylamino(methyl)carbamoyl]piperidin-1-yl]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-methylpropanamide |
| CAS | 249921-19-5 |
(3R)-1-(2-Methylalanyl-D-tryptophyl)-3-(phenylmethyl)-3-piperidinecarboxylic acid 1,2,2-trimethylhydrazide - Physico-chemical Properties
| Molecular Formula | C31H42N6O3 |
| Molar Mass | 546.7 |
| Density | 1.214 |
| Melting Point | 132-134°C |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Appearance | Form Solid, color White to Off-White |
| Color | White to Off-White |
| pKa | 16.22±0.46(Predicted) |
| Storage Condition | Refrigerator |
| Physical and Chemical Properties | Bioactive Anamorelin (ONO-7643, RC-1291, ST-1291) are ghrelin receptor selective agonists with oral activity and high affinity. In HEK293/GRLN FLIPR experiment, EC50 is 0.74 nM. |
| Use | Anamorelin is a new ghrelin receptor agonist. In FLIPR detection, EC50 is 0.74 nM. |
| In vitro study | Anamerelin has a significant agonistic effect and binding activity on the auxin receptor, stimulating growth hormone release in vitro. By its activity, anamerelin has an appetite-promoting and anabolic effect. In the experiment of screening the activity of anamerelin, 10 μm of anamerelin has weak binding force to L-type calcium channel receptor, serotonin transporter and sodium ion channel, it is therefore highly selective for auxin receptors. By inhibiting NF-κB,anamorelin is able to reduce the growth of pro-inflammatory cytokines, preventing muscle lysis (inhibition of proteolysis). |
| In vivo study | In rats, Anamorelin significantly increased food intake and body weight in a concentration-dependent manner, with significant increases in growth hormone levels at doses of 10 mg/kg or 30 mg/kg. In pigs, growth hormone and IGF-1 levels were elevated after administration of anamorelin. Anamerelin is orally active and has a longer half-life in the body than ghrelin, which is about 7 hours. It stimulates neuroendocrine responses, induces large increases in appetite and rapid metabolism. The plasma clearance of radioisotope-labeled anamorelin indicates that the vast majority of anamorelin is excreted and secreted by the faeces (92%). Eating reduces the area under the curve (AUC, I .e. reduces the extent to which it is absorbed and utilized in vivo) of anamorelin. It is metabolized by CYP3A4. In mouse tumor models, such as lewis lung carcinoma and human Bronchioloalveolar carcinoma models, anamorelin does not promote tumor growth. |
(3R)-1-(2-Methylalanyl-D-tryptophyl)-3-(phenylmethyl)-3-piperidinecarboxylic acid 1,2,2-trimethylhydrazide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.829 ml | 9.146 ml | 18.292 ml |
| 5 mM | 0.366 ml | 1.829 ml | 3.658 ml |
| 10 mM | 0.183 ml | 0.915 ml | 1.829 ml |
| 5 mM | 0.037 ml | 0.183 ml | 0.366 ml |
Last Update：2024-01-02 23:10:35
(3R)-1-(2-Methylalanyl-D-tryptophyl)-3-(phenylmethyl)-3-piperidinecarboxylic acid 1,2,2-trimethylhydrazide - Uses and synthesis methods
Target
Target Value
ghrelin receptor
(HEK293/GRLN FLIPR assay) 0.74 nM(EC50)
in vitro studies
Anamorelin has significant agonistic effect and binding activity on auxin receptor, stimulating the release of growth hormone in vitro. Through its activity, anamorelin has the effects of promoting appetite and promoting anabolism. In the experiment of screening anamorelin activity, 10 μM anamorelin has weak binding force to L-type calcium channel receptor, serotonin transporter and sodium ion channel, so it has high selectivity to auxin receptor. By inhibiting NF-& kappa;B,anamorelin can reduce the growth of pro-inflammatory cytokines and prevent myolysis (inhibition of proteolysis).
In vivo studies
in rats, Anamorelin can significantly increase food intake and body weight in a concentration-dependent manner, and at a dose of 10 mg/kg or 30 mg/kg, the level of growth hormone can be significantly increased. In pigs, after anamorelin administration, growth hormone and IGF-1 levels increase. Anamorelin has oral activity and has a longer half-life in the body than ghrelin, about 7 hours. It can stimulate neuroendocrine response, induce appetite increase and rapid metabolism. The plasma clearance of radioisotope-labeled anamorelin shows that the vast majority of anamorelin is excreted and secreted through excreta (92%). Eating will reduce the area under the curve of the anamorelin (AUC, that is, the degree to which it is absorbed and utilized in the body). It is metabolized by CYP3A4. In mouse tumor models, such as lewis lung cancer and human bronchioloalveolar carcinoma models, anamorelin do not promote tumor growth.
Last Update：2024-04-10 22:29:15
(3R)-1-(2-Methylalanyl-D-tryptophyl)-3-(phenylmethyl)-3-piperidinecarboxylic acid 1,2,2-trimethylhydrazide - Reference Information
| biological activity | anamerelin (ONO-7643, RC-1291, ST-1291), A high affinity ghrelin receptor selective agonist with an EC50 of 0.74 nM in the HEK293/GRLN FLIPR experiment. |
| Target | TargetValue ghrelin receptor (HEK293/GRLN FLIPR assay) 0.74 nM(EC50) |
| Target | Value |
| ghrelin receptor (HEK293/GRLN FLIPR assay) | 0.74 nM(EC50) |
| In vitro studies | Anamorelin has significant agonistic and binding activity to the auxin receptor, stimulating growth hormone release in vitro. By its activity, anamerelin has an appetite-promoting and anabolic effect. In the experiment of screening the activity of anamerelin, 10 μm of anamerelin has weak binding force to L-type calcium channel receptor, serotonin transporter and sodium ion channel, it is therefore highly selective for auxin receptors. By inhibiting NF-κB,anamorelin is able to reduce the growth of pro-inflammatory cytokines, preventing muscle lysis (inhibition of proteolysis). |
| in vivo studies | in rats, Anamorelin significantly and concentration-dependently increased food intake and body weight, at doses of 10 mg/kg or 30 mg/kg, growth hormone levels were significantly increased. In pigs, growth hormone and IGF-1 levels were elevated after administration of anamorelin. Anamerelin is orally active and has a longer half-life in the body than ghrelin, which is about 7 hours. It stimulates neuroendocrine responses, induces large increases in appetite and rapid metabolism. The plasma clearance of radioisotope-labeled anamorelin indicates that the vast majority of anamorelin is excreted and secreted by the faeces (92%). Eating reduces the area under the curve (AUC, I .e. reduces the extent to which it is absorbed and utilized in vivo) of anamorelin. It is metabolized by CYP3A4. In mouse tumor models, such as lewis lung carcinoma and human Bronchioloalveolar carcinoma models, anamorelin does not promote tumor growth. |
Last Update：2024-04-09 19:05:05
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Product Name: Anamorelin Visit Supplier Webpage Request for quotationCAS: 249921-19-5
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: Anamorelin Visit Supplier Webpage Request for quotationCAS: 249921-19-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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