[CAS NO. 249921-19-5] Anamorelin

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PRODUCTS SPECIFICATIONS [249921-19-5]

Catalog

HY-14734

Brand

MCE

CAS

249921-19-5

DESCRIPTION [249921-19-5]

Overview

MDL	-
Molecular Weight	546.70
Molecular Formula	C31H42N6O3
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

For research use only. We do not sell to patients.

5 Publications Citing Use of MCE

Summary

Anamorelin (RC-1291) is a potent ghrelin receptor agonist with EC ₅₀ value of 0.74 nM in the FLIPR assay.

IC50 & Target

Ki: 0.7 nM (ghrelin receptor) ^[1]
EC50: 0.74 nM (ghrelin receptor) ^[1]

In Vitro

In the FLIPR assay, Anamorelin (ANAM) shows significant agonist activity on the ghrelin receptor, with EC ₅₀ 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 (K _i ) of 0.70 nM. In the competition assay with radiolabeled ibutamoren ( ³⁵ S-MK-677; another ghrelin receptor agonist) Anamorelin (ANAM) is also found to bind with high affinity to the ghrelin receptor (IC ₅₀ =0.69 nM). In rat pituitary cells incubated with Anamorelin, there is a dose-dependent stimulatory effect on GH release and the potency (EC ₅₀ ) 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 (NK ₂ ) site (IC ₅₀ =0.021 μM); however, a subsequent NK ₂ functional assay demonstrates no functional activity ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 AUC _0-6h in rats ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00219817	Helsinn Therapeutics (U.S.), Inc	Cancer Cachexia	June 2005	Phase 2
NCT01395914	Helsinn Therapeutics (U.S.), Inc	Cachexia\|Non-Small Cell Lung Cancer	July 2011	Phase 3
NCT00267358	Helsinn Therapeutics (U.S.), Inc	Cancer Cachexia	November 2005	Phase 2
NCT04844970	Lahey Clinic\|Helsinn Healthcare SA\|Quartesian LLC	Metastatic Pancreatic Cancer	September 30, 2022	Phase 2
NCT01387269	Helsinn Therapeutics (U.S.), Inc	Cachexia\|Non-Small Cell Lung Cancer	July 2011	Phase 3
NCT00622193	Helsinn Therapeutics (U.S.), Inc	Carcinoma, Non-Small-Cell Lung	March 2008	Phase 2
NCT03035409	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Advanced Malignant Solid Neoplasm\|C-Reactive Protein Measurement\|Cancer Fatigue\|Metastatic Malignant Solid Neoplasm\|Recurrent Malignant Solid Neoplasm\|Weight Loss	February 8, 2017	Phase 2
NCT04021706	Tufts University\|National Institute of Arthritis and Musculoskeletal and Skin Diseases (NIAMS)	Sarcopenia\|Osteopenia	December 5, 2019	Phase 1
NCT03743051	Helsinn Healthcare SA	Cachexia; Cancer\|Non Small Cell Lung Cancer	December 18, 2018	Phase 3
NCT01505764	VA Office of Research and Development\|Helsinn Therapeutics (U.S.), Inc	Cancer Cachexia	June 2012	Phase 2
NCT03637816	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Anorexia\|Lung Non-Small Cell Carcinoma\|Stage III Lung Cancer AJCC v8\|Stage IIIA Lung Cancer AJCC v8\|Stage IIIB Lung Cancer AJCC v8\|Stage IIIC Lung Cancer AJCC v8\|Stage IV Lung Cancer AJCC v8\|Stage IVA Lung Cancer AJCC v8\|Stage IVB Lung Cancer AJCC v8	November 27, 2018	Phase 2\|Phase 3
NCT00378131	Helsinn Therapeutics (U.S.), Inc	Cancer Cachexia	September 2006	Phase 2
NCT01387282	Helsinn Therapeutics (U.S.), Inc	Cachexia\|Non-Small Cell Lung Cancer	July 2011	Phase 3
NCT03743064	Helsinn Healthcare SA	Cachexia; Cancer\|Non Small Cell Lung Cancer	December 18, 2018	Phase 3

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL ( 182.92 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent 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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

* All of the co-solvents are available by MCE.

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.

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