AnamorelinGhrelin receptor agonist, synthetic, orally active CAS# 249921-19-5 |
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Quality Control & MSDS
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| Cas No. | 249921-19-5 | SDF | Download SDF |
| PubChem ID | 9828911 | Appearance | Powder |
| Formula | C31H42N6O3 | M.Wt | 546.7 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | RC-1291; ONO-7643 | ||
| Solubility | DMSO : ≥ 100 mg/mL (182.92 mM) *"≥" means soluble, but saturation unknown. | ||
| 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 | ||
| SMILES | CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCCC(C3)(CC4=CC=CC=C4)C(=O)N(C)N(C)C)N | ||
| Standard InChIKey | VQPFSIRUEPQQPP-MXBOTTGLSA-N | ||
| Standard InChI | 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 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Anamorelin is a novel ghrelin receptor agonist with EC50 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 EC50 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 (Ki) of 0.70 nM. 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=0.69 nM). In rat pituitary cells incubated with Anamorelin, there is a dose-dependent stimulatory effect on GH release and the potency (EC50) 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 (NK2) site (IC50=0.021 μM); however, a subsequent NK2 functional assay demonstrates no functional activity[1].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 AUC0-6h in rats[1]. References: | |||||
Anamorelin Dilution Calculator
Anamorelin Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.8292 mL | 9.1458 mL | 18.2916 mL | 36.5831 mL | 45.7289 mL |
| 5 mM | 0.3658 mL | 1.8292 mL | 3.6583 mL | 7.3166 mL | 9.1458 mL |
| 10 mM | 0.1829 mL | 0.9146 mL | 1.8292 mL | 3.6583 mL | 4.5729 mL |
| 50 mM | 0.0366 mL | 0.1829 mL | 0.3658 mL | 0.7317 mL | 0.9146 mL |
| 100 mM | 0.0183 mL | 0.0915 mL | 0.1829 mL | 0.3658 mL | 0.4573 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
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Evidence for partial pharmaceutical reversal of the cancer anorexia-cachexia syndrome: the case of anamorelin.[Pubmed:26675382]
J Cachexia Sarcopenia Muscle. 2015 Dec;6(4):275-7.
A major component of the cancer anorexia-cachexia syndrome is a decline in food intake. Up until now none of the drugs that improve appetite also improve skeletal muscle. Recent studies have suggested that the oral ghrelin-analog, Anamorelin, increased food intake and muscle mass. Unfortunately, it does not increase muscle power. Its regulatory future is uncertain, although it has important clinical effects.
Anamorelin in patients with non-small-cell lung cancer and cachexia (ROMANA 1 and ROMANA 2): results from two randomised, double-blind, phase 3 trials.[Pubmed:26906526]
Lancet Oncol. 2016 Apr;17(4):519-531.
BACKGROUND: Patients with advanced cancer frequently experience anorexia and cachexia, which are associated with reduced food intake, altered body composition, and decreased functionality. We assessed Anamorelin, a novel ghrelin-receptor agonist, on cachexia in patients with advanced non-small-cell lung cancer and cachexia. METHODS: ROMANA 1 and ROMANA 2 were randomised, double-blind, placebo-controlled phase 3 trials done at 93 sites in 19 countries. Patients with inoperable stage III or IV non-small-cell lung cancer and cachexia (defined as >/=5% weight loss within 6 months or body-mass index <20 kg/m(2)) were randomly assigned 2:1 to Anamorelin 100 mg orally once daily or placebo, with a computer-generated randomisation algorithm stratified by geographical region, cancer treatment status, and weight loss over the previous 6 months. Co-primary efficacy endpoints were the median change in lean body mass and handgrip strength over 12 weeks and were measured in all study participants (intention-to-treat population). Both trials are now completed and are registered with ClinicalTrials.gov, numbers NCT01387269 and NCT01387282. FINDINGS: From July 8, 2011, to Jan 28, 2014, 484 patients were enrolled in ROMANA 1 (323 to Anamorelin, 161 to placebo), and from July 14, 2011, to Oct 31, 2013, 495 patients were enrolled in ROMANA 2 (330 to Anamorelin, 165 to placebo). Over 12 weeks, lean body mass increased in patients assigned to Anamorelin compared with those assigned to placebo in ROMANA 1 (median increase 0.99 kg [95% CI 0.61 to 1.36] vs -0.47 kg [-1.00 to 0.21], p<0.0001) and ROMANA 2 (0.65 kg [0.38 to 0.91] vs -0.98 kg [-1.49 to -0.41], p<0.0001). We noted no difference in handgrip strength in ROMANA 1 (-1.10 kg [-1.69 to -0.40] vs -1.58 kg [-2.99 to -1.14], p=0.15) or ROMANA 2 (-1.49 kg [-2.06 to -0.58] vs -0.95 kg [-1.56 to 0.04], p=0.65). There were no differences in grade 3-4 treatment-related adverse events between study groups; the most common grade 3-4 adverse event was hyperglycaemia, occurring in one (<1%) of 320 patients given Anamorelin in ROMANA 1 and in four (1%) of 330 patients given Anamorelin in ROMANA 2. INTERPRETATION: Anamorelin significantly increased lean body mass, but not handgrip, strength in patients with advanced non-small-cell lung cancer. Considering the unmet medical need for safe and effective treatments for cachexia, Anamorelin might be a treatment option for patients with cancer anorexia and cachexia. FUNDING: Helsinn Therapeutics.
Anamorelin for cancer anorexia-cachexia syndrome: a systematic review and meta-analysis.[Pubmed:28074289]
Support Care Cancer. 2017 May;25(5):1651-1659.
PURPOSE: The aim of this study was to evaluate the therapeutic effects of Anamorelin on patients with cancer anorexia-cachexia syndrome (CACS) based on a meta-analysis of published randomized trials. METHODS: We searched PubMed, Embase, Medline, and the Cochrane Central Register of Controlled Trials databases. Data from each selected study were evaluated individually. All continuous outcomes were calculated by the mean difference or standardized mean difference with 95% confidence interval for each study. Heterogeneity was assessed by using the Chi(2) test at a significance level of P < 0.1, in addition to the I (2) statistic (I (2) > 50% indicated substantial heterogeneity). RESULT: At last, four studies were included from 284 records. In three studies, lean body mass was reported and there was a significant difference between placebo and Anamorelin groups (P < 0.00001), without significant heterogeneity (I (2) = 0%). All the four studies reported the body weight change from baseline, and there was significant difference between placebo and Anamorelin groups (P = 0.007), but with high heterogeneity (I (2) = 97%). Two studies reported Anderson Symptom Assessment Scale (ASAS) score, and Anamorelin significantly increased the total ASAS score of CACS patients (P < 0.00001), without any heterogeneity (I (2) = 0%). Three studies reported non-dominant handgrip strength, and there was no significant difference between Anamorelin and placebo groups (P = 0.16). Three studies reported insulin-like growth factor-1 level, and there was significant difference between Anamorelin and placebo groups (P = 0.02), but with high heterogeneity (I (2) = 96%). Three studies reported IGF binding protein-3 concentration. Anamorelin significantly increased such concentration compared with placebo did (P < 0.00001). However, there was still higher heterogeneity (I (2) = 59%). All the included studies reported adverse events. Compared with placebo, Anamorelin induced fewer adverse events, but there was no significant difference between the two groups (RR = 0.07, P = 0.35). CONCLUSION: In the included studies, Anamorelin had some positive effects to relieve the symptoms and improved the quality of life. However, the heterogeneity was apparent, so the clinical effects of Anamorelin should be further validated by increasing the sample size, varying the range of doses during treatment, and observing other outcomes. We are still confident for the future application of Anamorelin in phase III clinical trials.
Anamorelin (ONO-7643) in Japanese patients with non-small cell lung cancer and cachexia: results of a randomized phase 2 trial.[Pubmed:27005463]
Support Care Cancer. 2016 Aug;24(8):3495-505.
PURPOSE: Cancer cachexia is characterized by decreased body weight (mainly lean body mass [LBM]) and negatively impacts quality of life (QOL) and prognosis. Anamorelin (ONO-7643) is a novel selective ghrelin receptor agonist under development for treating cancer cachexia. METHODS: In this double-blind, exploratory phase 2 trial, we examined the efficacy and safety of Anamorelin in Japanese patients (n = 181) with non-small cell lung cancer (NSCLC) and cancer cachexia (>/=5 % weight loss within the previous 6 months). The participants were randomized into three groups and were administered 50 or 100 mg Anamorelin, or placebo, orally every day for 12 weeks. The co-primary endpoints were the changes from baseline over 12 weeks in LBM and handgrip strength (HGS). Secondary endpoints included body weight, QOL, Karnofsky Performance Scale (KPS), and serum biomarkers. RESULTS: The change in LBM over 12 weeks was 0.55 and 1.15 kg in the placebo and 100-mg Anamorelin groups, respectively, but the efficacy of Anamorelin in HGS was not detected. The changes in body weight were -0.93, 0.54, and 1.77 kg in the placebo, 50-mg Anamorelin, and 100-mg Anamorelin groups, respectively. Anamorelin (100 mg) significantly improved KPS and QOL-ACD compared with placebo. Administration of Anamorelin for 12 weeks was well tolerated. CONCLUSIONS: This phase 2 study showed that 100 mg Anamorelin has promising results in improving lean body mass, performance status, and especially, QOL in patients with cancer cachexia.
