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Purity: ≥98%
Anamorelin (formerly also known as RC-1291 and ONO-7643) is a novel, potent, and orally bioavailable ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay. It is a small-molecule ghrelin mimetic that has both anabolic and appetite-stimulating properties. Anamorelin mimics the appetite-stimulating and growth hormone-releasing properties of grhelin by binding to and stimulating the growth hormone secretagogue receptor (GHSR) centrally. In addition to potentially reducing the production of pro-inflammatory cytokines TNF-alpha and interleukin-6, stimulation of GHSR may also directly contribute to appetite loss associated with cancer.
| Targets |
ghrelin receptor ( Ki = 0.7 nM ); ghrelin receptor ( EC50 = 0.74 nM )
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| ln Vitro |
Anamorelin (ANAM) exhibits strong agonist activity on the ghrelin receptor in the FLIPR assay, with an EC50 value of 0.74 nM. Anamorelin exhibits negligible antagonistic effects at 1,000 nM and higher concentrations. Anamorelin exhibits a binding affinity constant (Ki) of 0.70 nM for the ghrelin receptor in the binding experiments. Anamorelin (ANAM) is also shown to bind to the ghrelin receptor with a high affinity in the competition assay using radiolabeled ibutamoren (IC50=0.69 nM). Anamorelin has a dose-dependent stimulatory effect on GH release in rat pituitary cells, and its potency (EC50) is 1.5 nM. Anamorelin is tested for its ability to bind to more than 100 different receptors, ion channels, transporters, and enzymes. An NK2 functional assay shows no functional activity, despite anamorelin's demonstrated binding to the tachykinin neurokinin 2 (NK2) site (IC50=0.021 μM).
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| ln Vivo |
Anamorelin (ANAM) increases food intake and body weight in rats from Day 2 to Day 7 of treatment significantly when given orally at a dose of 3, 10, or 30 mg/kg once daily, in comparison to the vehicle control. Each dose level causes a dose-dependent cumulative change in food intake and weight gain, which is significant (P<0.05) when compared to the control at all dose levels. A dose-dependent rise in plasma GH levels and GH AUC0-6h is observed in rats administered a single oral dose of 3, 10, or 30 mg/kg of anamorelin[1].
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| Enzyme Assay |
In the competition assay, membranes are supplemented with 35S-MK-677 and anamorelin (ANAM) concentrations ranging from 1 pM to 10 μM. To ascertain nonspecific binding, 10 μM nonlabeled MK-677 is added. The samples are applied to GF/B filters, which have been pretreated with 0.5% PEI, and the mixture is incubated at 30°C for 60 minutes. The filters are then counted using an OptiPhase counter after being cleaned in 0.9% NaCl[1].
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| Animal Protocol |
Rats: Rats are separated into four groups for the purpose of assessing food intake and body weight: Anamorelin 3 mg/kg (n = 7), 10 mg/kg (n = 7), or 30 mg/kg (n = 7), or vehicle control (n = 8). 100 μL blood samples are taken prior to and 0.25, 0.5, 1, 2, 3, 4, 5, and 6 hours following a single dose. Rats are put to sleep using a 64.8 mg/kg dose of sodium pentobarbital. In order to collect blood, a catheter equipped with a three-way cock to allow extra blood to return, an extension tube, and a 1 mL sampling syringe is placed inside the left femoral artery and filled with heparinized saline solution. A Rat Growth Hormone EIA kit and microplate reader are used to immunochemically measure the levels of growth hormone in plasma. There are two measurement takes place. The time course of GH plasma concentrations is assessed, as well as the area under the GH concentration curve from 0 to 6 hours (AUC0-6h) postdose.
Pig: Anamorelin is administered intraperitoneally (IDI) using a dosing catheter to six groups of pigs each. Blood is drawn for the GH stimulation profile at 15, 30, 45, 60, and 120 minutes after dosing, as well as at 30 and 15 minutes before. The animals were given either a single dose (3.5 mg/kg) or a once-daily administration (1 mg/kg) of anamorelin for seven days. Following the first and seventh doses, stimulation profiles were taken. In order to measure IGF-1 levels, pigs are given either a placebo or anamorelin (1 mg/kg/day) for seven days, after which they switch between the two treatments for an additional seven days. Every day, right before the dose, a single blood sample is obtained. |
| References |
| Molecular Formula |
C31H42N6O3
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|---|---|
| Molecular Weight |
546.70359
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| Exact Mass |
546.33
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| Elemental Analysis |
C, 63.85; H, 7.43; Cl, 6.08; N, 14.41; O, 8.23
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| CAS # |
249921-19-5
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| Related CAS # |
Anamorelin hydrochloride; 861998-00-7; Anamorelin Fumarate; 339539-92-3; 249921-19-5
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| Appearance |
white to off-white solid powder
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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
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| InChi Key |
VQPFSIRUEPQQPP-MXBOTTGLSA-N
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| InChi Code |
InChI=1S/C31H42N6O3/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)/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
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| Synonyms |
ONO7643; ONO-7643; ONO 7643; RC 1291; RC1291; RC-1291
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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 |
| 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: ~100 mg/mL (~182.9 mM)
Ethanol: ~50 mg/mL |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8292 mL | 9.1458 mL | 18.2916 mL | |
| 5 mM | 0.3658 mL | 1.8292 mL | 3.6583 mL | |
| 10 mM | 0.1829 mL | 0.9146 mL | 1.8292 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 |
| NCT03637816 | Active Recruiting |
Drug: Anamorelin Hydrochloride Other: Placebo |
Stage III Lung Cancer AJCC v8 Anorexia |
M.D. Anderson Cancer Center | November 27, 2018 | Phase 2 Phase 3 |
| NCT03035409 | Active Recruiting |
Drug: Anamorelin Hydrochloride Other: Nutritional Assessment |
Cancer Fatigue Weight Loss |
M.D. Anderson Cancer Center | February 8, 2017 | Phase 2 |
| NCT04844970 | Completed | Drug: Anamorelin Hydrochloride Drug: Placebo |
Metastatic Pancreatic Cancer | Lahey Clinic | April 1, 2023 | Phase 2 |
| NCT03743064 | Completed | Drug: anamorelin HCl Drug: Placebo Oral Tablet |
Non Small Cell Lung Cancer Cachexia; Cancer |
Helsinn Healthcare SA | December 18, 2018 | Phase 3 |
| NCT03743051 | Completed | Drug: Anamorelin Hydrochloride Drug: Placebo Oral Tablet |
Non Small Cell Lung Cancer Cachexia; Cancer |
Helsinn Healthcare SA | December 18, 2018 | Phase 3 |
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