Anamorelin

Catalog No.S4980 Synonyms: ONO-7643, RC-1291, ST-1291

For research use only.

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.

Anamorelin Chemical Structure

CAS No. 249921-19-5

Selleck's Anamorelin has been cited by 1 Publication

Purity & Quality Control

Choose Selective GHSR Inhibitors

Biological Activity

Description 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.
Targets
ghrelin receptor [2]
(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, anamorelin has both orexigenic and anabolic properties. In the screening for anamorelin activity, 10 μM Anamorelin 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[2]. By inhibiting nuclear factor κB, anamorelin reduces production of pro-inflammatory cytokines and stops muscle breakdown (inhibits proteolysis)[3].

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 anamorelin administration in pigs. Anamorelin 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[2]. 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 anamorelin by 4-fold. Metabolism occurs by CYP3A4. In mouse tumor models, such as Lewis lung and human bronchioalveolar carcinoma, anamorelin does not promote tumor growth[3].

Protocol (from reference)

Animal Research:

[1]

  • Animal Models: A549 NSCLC xenografts
  • Dosages: 3, 10, or 30 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 546.70
Formula

C31H42N6O3

CAS No. 249921-19-5
Storage 3 years -20°C powder
2 years -80°C in solvent
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

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

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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