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Anamorelin hydrochloride
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Anamorelin hydrochloride
CAS No. : 861998-00-7
MCE 站:Anamorelin hydrochloride
产品活性:Anamorelin (RC-1291) hydrochloride 是一种有效的 ghrelin receptor 激动剂,FLIPR 检测中,EC50 为 0.74 nM。
研究领域:GPCR/G Protein
作用靶点:GHSR
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.
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.
相关产品:Drug Repurposing Compound Library Plus | FDA-Approved Drug Library Plus | Bioactive Compound Library Plus | GPCR/G Protein Compound Library | FDA-Approved Drug Library | Anti-Cancer Compound Library | Drug Repurposing Compound Library | Endocrinology Compound Library | Anti-COVID-19 Compound Library | Orally Active Compound Library | FDA Approved & Pharmacopeial Drug Library | Ibutamoren Mesylate | Anamorelin | TC-G-1008 | Capromorelin Tartrate | TM-N1324 | Human growth hormone-releasing factor | L-692429 | Alexamorelin Met 1 | K-(D-1-Nal)-FwLL-NH2 | L-692585 | Obestatin(rat) | Ulimorelin
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热门标签:RC-1291 hydrochloride