| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
In the FLIPR test, anamorelin (ANAM) has strong agonist action at the ghrelin receptor, with an EC50 value of 0.74 nM. Anamorolin Up to 1,000 nM of the antagonist was not found to have any discernible activity. Anamorelin bonded to the ghrelin receptor in binding assays, exhibiting a binding affinity constant (Ki) of 0.70 nM. It was also shown that anamorelin (ANAM) binds to ghrelin receptors with high affinity (IC50=0.69 nM). Anamorelin, with a 1.5 nM potency, stimulates the release of growth hormone in rat pituitary cells in a dose-dependent manner. Anamorelin is tested for its ability to bind to over 100 different receptors, ion channels, transporters, and enzymes. The binding of anamorelin to the tachykinin neurokinin 2 (NK2) site (IC50=0.021 μM) was observed, but no functional activity was shown in subsequent NK2 experiments [1].
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| ln Vivo |
Anamorelin (ANAM) administered orally once daily at 3, 10, or 30 mg/kg in rats resulted in a significant increase in food intake and body weight from days 2 to 7 of therapy as compared to vehicle controls. When compared to controls, cumulative changes in food intake and weight gain increased with dose and were statistically significant at all dose levels (P<0.05). Rats' plasma GH levels and GH AUC0–6h increased in a dose-dependent manner after receiving a single oral dosage of 3, 10, or 30 mg/kg of anamorelin [1].
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| References | |
| Additional Infomation |
Anamorelin Hydrochloride is the orally bioavailable hydrochloride salt of a synthetic, small-molecule ghrelin mimetic with appetite-stimulating and anabolic activities. Anamorelin binds to and stimulates the growth hormone secretagogue receptor (GHSR) centrally, thereby mimicking the appetite-stimulating and growth hormone-releasing effects of grhelin. Stimulation of GHSR may also reduce the production of the pro-inflammatory cytokines TNF-alpha and interleukin-6, which may play a direct role in cancer-related loss of appetite.
See also: Anamorelin (annotation moved to). Drug Indication Treatment of anorexia, cachexia or unintended weight loss in adult patients with non-small cell lung cancer (NSCLC) Treatment of cancer related cachexia |
| Molecular Formula |
C31H43CLN6O3
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|---|---|
| Molecular Weight |
583.2
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| Exact Mass |
582.308
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| CAS # |
861998-00-7
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| Related CAS # |
Anamorelin;249921-19-5;Anamorelin Fumarate;339539-92-3
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| PubChem CID |
16072155
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| Appearance |
White to off-white solid powder
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| LogP |
4.999
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
41
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| Complexity |
904
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| Defined Atom Stereocenter Count |
2
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| 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
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| InChi Key |
VFYAEUWJFGTGGO-GHTUPXNNSA-N
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| InChi Code |
InChI=1S/C31H42N6O3.ClH/c1-30(2,32)28(39)34-26(18-23-20-33-25-15-10-9-14-24(23)25)27(38)37-17-11-16-31(21-37,29(40)36(5)35(3)4)19-22-12-7-6-8-13-22;/h6-10,12-15,20,26,33H,11,16-19,21,32H2,1-5H3,(H,34,39);1H/t26-,31-;/m1./s1
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| Chemical Name |
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;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~170 mg/mL (~291.52 mM)
H2O : ~50 mg/mL (~85.74 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (8.57 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (8.57 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (8.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7147 mL | 8.5734 mL | 17.1468 mL | |
| 5 mM | 0.3429 mL | 1.7147 mL | 3.4294 mL | |
| 10 mM | 0.1715 mL | 0.8573 mL | 1.7147 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01395914 | Completed | Drug: Anamorelin HCl Drug: Placebo |
Cachexia Non-Small Cell Lung Cancer |
Helsinn Therapeutics (U.S.), Inc | 2011-07 | Phase 3 |
| NCT01505764 | Terminated | Drug: Anamorelin HCl Drug: Placebo |
Cancer Cachexia | VA Office of Research and Development | 2012-06 | Phase 2 |
| NCT03743064 | Completed | Drug: anamorelin HCl Drug: Placebo Oral Tablet |
Cachexia; Cancer Non Small Cell Lung Cancer |
Helsinn Healthcare SA | 2019-05-06 | Phase 3 |
| NCT04844970 | Recruiting | Drug: Anamorelin Hydrochloride Drug: Placebo |
Metastatic Pancreatic Cancer | Lahey Clinic | 2023-04-01 | Phase 2 |
| NCT03743051 | Completed | Drug: Anamorelin Hydrochloride Drug: Placebo Oral Tablet |
Cachexia; Cancer Non Small Cell Lung Cancer |
Helsinn Healthcare SA | 2019-03-05 | Phase 3 |
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