Anamorelin (hydrochloride)

861998-00-7

C31H43ClN6O3

DMSO : >= 28 mg/mL (48.01 mM)

GPCR/G Protein

Anamorelin hydrochloride is a novel ghrelin receptor agonist with EC₅₀ 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 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 (K_i) 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 uM); however, a subsequent NK₂ functional assay demonstrates no functional activity^[1]. 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].