Name: Anamorelin Fumarate
Brand: GlpBio
SKU: GC35337
Availability: InStock
Rating: 5 (36 reviews)

GlpBio Products Cited In Reputable Papers

Nature
610.7931 (2022): 366-372

Nature
618, 1017–1023 (2023)

Cell
183.7 (2020): 1867-1883

Cell Research
31, 1291–1307 (2021)

Cell Research
33, 273–287 (2023)

Cell Research
33, 546–561 (2023)

Molecular Cancer
21.1 (2022): 1-17

Molecular Cancer
21.1 (2022): 1-18

Cancer Cell
39 (2021): 1-16

Cell Host Microbe
30.8 (2022): 1124-1138

Cell Host Microbe
31.5 (2023): 766-780

Cell Host Microbe
31.3 (2023): 418-43

Cell Metabolism
34.2 (2022): 240-255

Ann Rheum Dis
82(4): 533-545 (2023)

Cell Mol Immunol
20, 264–276 (2023)

Adv Funct Mater
33.35 (2023): 2214998

Product Documents

Quality Control & SDS

View current batch:

Purity: >98.00%

Protocol

Kinase experiment:

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 experiment:

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 is a novel ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay. Ki: 0.7 nM (ghrelin receptor)[1]EC50: 0.74 nM (ghrelin receptor)[1]

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 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].

[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.

Cas No.	339539-92-3	SDF
Canonical SMILES	[H][C@](CC1=CNC2=CC=CC=C21)(NC(C(C)(C)N)=O)C(N3CCC[C@@](C(N(C)N(C)C)=O)(CC4=CC=CC=C4)C3)=O.O=C(O)/C=C/C(O)=O
Formula	C₃₅H₄₆N₆O₇	M.Wt	662.78
Solubility	Soluble in DMSO	Storage	Store at -20°C
General tips	Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition	Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
		1 mg	5 mg	10 mg
	1 mM	1.5088 mL	7.544 mL	15.088 mL
	5 mM	0.3018 mL	1.5088 mL	3.0176 mL
	10 mM	0.1509 mL	0.7544 mL	1.5088 mL

Molarity Calculator
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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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