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Anamorelin GHSR agonist

Name: Anamorelin
Brand: Selleck Chemicals
SKU: S4980
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S4980

Anamorelin (ONO-7643, RC-1291, ST-1291) is an orally active, high-affinity, selective agonist of the ghrelin receptor with an EC50 value of 0.74 nM in the HEK293/GRLN FLIPR assay.

Chemical Structure

Molecular Weight: 546.70

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Quality Control

Batch: Purity: 99.93%

99.93

Related Targets	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Other GHSR Inhibitors	AnaMorelin hydrochloride

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (182.91 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 50 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.15mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.410mg/ml (0.75mM)	Taking the 1 mL working solution as an example, add 50 μL of 8.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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

Dosing volume per animal: μL

Number of animals:

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

% DMSO

Calculation results:

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.

Chemical Information, Storage & Stability

Molecular Weight	546.70	Formula	C₃₁H₄₂N₆O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	249921-19-5	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	ONO-7643, RC-1291, ST-1291			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

Mechanism of Action

Targets/IC₅₀/Ki	ghrelin receptor (HEK293/GRLN FLIPR assay) 0.74 nM(EC50)
In vitro	Anamorelin shows significant agonist and binding activity on the ghrelin receptor, and stimulates growth hormone (GH) release in vitro. Through its ghrelin and GH-releasing activity, this compound has both orexigenic and anabolic properties. In the screening for its activity, 10 μM of this chemical shows weak binding to the calcium channel L-type receptors, the serotonin transporter, and the sodium channel. Therefore, it exhibits a high selectivity versus ghrelin receptors. By inhibiting nuclear factor κB, this agent reduces production of pro-inflammatory cytokines and stops muscle breakdown (inhibits proteolysis).
In vivo	In rats, Anamorelin significantly and dose-dependently increases food intake and body weight at all dose levels compared with control, and significantly increased growth hormone (GH) levels at 10 or 30 mg/kg doses. Growth hormone and IGF-1 levels increase following this compound administration in pigs. It is orally active and has a longer half-life (approximately 7 h) than ghrelin. It stimulates neuroendocrine responses and can induce rapid positive effects on appetite and metabolism. Plasma clearance of radiolabelled anamorelin shows that most of the drug is excreted in the feces (92%). Food decreases the area under the curve (AUC) of this chemical by 4-fold. Metabolism occurs by CYP3A4. In mouse tumor models, such as Lewis lung and human bronchioalveolar carcinoma, it does not promote tumor growth.
References	[1] https://pubmed.ncbi.nlm.nih.gov/23579947/ [2] https://pubmed.ncbi.nlm.nih.gov/25267366/

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