Anamorelin hydrochloride

Cas No.:	861998-00-7
Chemical Name:	Anamorelin hydrochloride
Synonyms:	UNII-55F75LJQ0V;Anamorelin hydrochloride;RC 1291 hydrochloride;ONO 7643 hydrochloride;ONO-7643 hydrochloride;SureCN4535148;2-amino-N-[(2R)-1-[(3R)-3-benzyl-3-[dimethylamino(methyl)carbamoyl]piperidin-1-yl]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-methylpropanamide,hydrochloride;ANAMORELIN HCL;2-amino-N-[(2R)-1-[(3R)-3-benzyl-3-[dimethylamino(methyl)carbamoyl]piperidin-1-yl]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-methylpropanamide;hydrochloride;RC-1291 hydrochloride;3-Piperidinecarboxylic acid, 1-(2-methylalanyl-D-tryptophyl)-3-(phenylmethyl)-, trimethylhydrazide, monohydrochloride, (3R)- (9CI);Adlumiz;RC 1291 HCl;AC-29222;F84877;RC-1291 hydrochloride;ONO-7643 hydrochloride;Anamorelin hydrochloride (JAN/USAN);Anamorelin hydrochloride [USAN];ANAMORELIN HYDROCHLORIDE [WHO-DD];861998-00-7;D08856;RC-1291 HCL;55F75LJQ0V;CHEMBL2103794;2-amino-N-[(2R)-1-[(3R)-3-benzyl-3-[dimethylamino(methyl)carbamoyl]piperidin-1-yl]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-methylpropanamide;hydrochloride;CS-1037;MS-30447;(3R)-1-(2-Methylalanyl-D-tryptophyl)-3-(phenylmethyl)-3-piperidinecarboxylic Acid Trimethylhydrazide Monohydrochloride; RC 1291 HCl; RC 1291 Hydrochloride;Adlumiz (TN);MFCD23098788;SCHEMBL4535148;(3R)-1-((2R)-2-((2-Amino-2-methylpropanoyl)amino)-3-(indol-3-yl)propanoyl)-3-benzyl-N,N',N'-trimethylpiperidine-3-carbohydrazide hydrochloride;AKOS030526940;Anamorelin hydrochloride?;Anamorelin?;BCP15207;DA-70837;ANAMORELIN HYDROCHLORIDE [MI];ANAMORELIN HYDROCHLORIDE [JAN];2-Amino-N-((R)-1-((R)-3-benzyl-3-(1,2,2-trimethylhydrazine-1-carbonyl)piperidin-1-yl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-2-methylpropanamide hydrochloride;Anamorelin (hydrochloride);Q27261306;DTXSID70235443;3-Piperidinecarboxylic acid, 1-(2-methylalanyl-D-tryptophyl)-3-(phenylmethyl)-, trimethylhydrazide, monohydrochloride, (3R)-;HY-14734A
SMILES:	C(C1C=CC=CC=1)[C@@]1(CCCN(C(=O)[C@H](NC(=O)C(N)(C)C)CC2=CNC3C=CC=CC2=3)C1)C(=O)N(C)N(C)C.Cl
Formula:	C31H43ClN6O3
M.Wt:	583.164526224136
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	Anamorelin hydrochloride is a novel ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay.
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 AUC0-6h in rats[1].
In Vitro:	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].