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Anamorelin Fumarate

GHSR stimulator CAS# 339539-92-3

Anamorelin Fumarate

Catalog No. BCC1363----Order now to get a substantial discount!

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Chemical structure

Anamorelin Fumarate

3D structure

Chemical Properties of Anamorelin Fumarate

Cas No. 339539-92-3 SDF Download SDF
PubChem ID 71576657 Appearance Powder
Formula C35H46N6O7 M.Wt 662.78
Type of Compound N/A Storage Desiccate at -20°C
Synonyms ONO-7643 Fumarate; RC1291 Fumarate
Solubility Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc.
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;(E)-but-2-enedioic acid
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.C(=CC(=O)O)C(=O)O
Standard InChIKey RJIOUAKEXOTTOG-LUDSMFHYSA-N
Standard InChI InChI=1S/C31H42N6O3.C4H4O4/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;5-3(6)1-2-4(7)8/h6-10,12-15,20,26,33H,11,16-19,21,32H2,1-5H3,(H,34,39);1-2H,(H,5,6)(H,7,8)/b;2-1+/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.
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.
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.

Biological Activity of Anamorelin Fumarate

DescriptionAnamorelin Fumarate 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:
[1]. Pietra C, et al. Anamorelin HCl (ONO-7643), a novel ghrelin receptor agonist, for the treatment of cancer anorexia-cachexiasyndrome: preclinical profile. J Cachexia Sarcopenia Muscle. 2014 Dec;5(4):329-37.

Protocol

Kinase Assay [1]
For the competition assay, Anamorelin (ANAM) concentrations (1 pM-10 μM) are added to the membranes together with 35S-MK-677. Nonspecific binding is determined by adding 10 μM nonlabeled MK-677. The mixture is incubated at 30°C 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[1].

Animal Administration [1]
Rats[1] For the assessment of food intake and body weight, rats are divided into four groups: Anamorelin 3 mg/kg (n=7), 10 mg/kg (n=7), or 30 mg/kg (n=7), or vehicle control (n=8), and 100 μL blood samples are collected before and 0.25, 0.5, 1, 2, 3, 4, 5, and 6 h after single dosing. Rats are anesthetized with sodium pentobarbital 64.8 mg/kg. A catheter filled with heparinized saline solution is inserted in the left femoral artery for blood collection and fitted with an extension tube, 1 mL 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 6 h (AUC0-6h) postdose and the time course of GH plasma concentrations are evaluated. Pig[1] 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 (3.5 mg/kg), or once-daily administration (1 mg/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 (1 mg/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.

References:
[1]. Pietra C, et al. Anamorelin HCl (ONO-7643), a novel ghrelin receptor agonist, for the treatment of cancer anorexia-cachexiasyndrome: preclinical profile. J Cachexia Sarcopenia Muscle. 2014 Dec;5(4):329-37.

Anamorelin Fumarate Dilution Calculator

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Anamorelin Fumarate Molarity Calculator

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Preparing Stock Solutions of Anamorelin Fumarate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.5088 mL 7.544 mL 15.088 mL 30.1759 mL 37.7199 mL
5 mM 0.3018 mL 1.5088 mL 3.0176 mL 6.0352 mL 7.544 mL
10 mM 0.1509 mL 0.7544 mL 1.5088 mL 3.0176 mL 3.772 mL
50 mM 0.0302 mL 0.1509 mL 0.3018 mL 0.6035 mL 0.7544 mL
100 mM 0.0151 mL 0.0754 mL 0.1509 mL 0.3018 mL 0.3772 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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Background on Anamorelin Fumarate

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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Description

Anamorelin Fumarate is a novel ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay.

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