[CAS NO. 249921-19-5] Anamorelin

Name: Anamorelin
Brand: Arctom Scientific
SKU: SLK-S4980

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PRODUCTS SPECIFICATIONS [249921-19-5]

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Catalog

SLK-S4980

Brand

Selleck

CAS

249921-19-5

DESCRIPTION [249921-19-5]

Overview

MDL	-
Molecular Weight	546.70
Molecular Formula	C31H42N6O3
SMILES	C([C@@]1(C(N(N(C)C)C)=O)CN(C([C@@H](CC=2C=3C(NC2)=CC=CC3)NC(C(C)(C)N)=O)=O)CCC1)C4=CC=CC=C4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.8292 mL	9.1458 mL	18.2916 mL
5 mM	0.3658 mL	1.8292 mL	3.6583 mL
10 mM	0.1829 mL	0.9146 mL	1.8292 mL
50 mM	0.0366 mL	0.1829 mL	0.3658 mL

Description

Anamorelin (ONO-7643, RC-1291, ST-1291) is an orally active, high-affinity, selective agonist of the 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. By inhibiting nuclear factor κB, anamorelin 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 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. 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.

References

[1] Northrup R, et al. Support Care Cancer. 2013, 21(9):2409-15.
[2] Pietra C, et al. J Cachexia Sarcopenia Muscle. 2014, 5(4):329-37.

Synonyms

3-Piperidinecarboxylic acid, 1-[(2R)-2-[(2-amino-2-methyl-1-oxopropyl)amino]-3-(1H-indol-3-yl)-1-oxopropyl]-3-(phenylmethyl)-, 1,2,2-trimethylhydrazide, (3R)-

3-Piperidinecarboxylic acid, 1-(2-methylalanyl-D-tryptophyl)-3-(phenylmethyl)-, trimethylhydrazide, (3R)-

RC 1291

Anamorelin