85-2073-07　Ghrelin Receptor Antagonist, JMV 2959 10mg　CAS No:925238-89-7　217382

特徴

• A 1, 2, 4-triazole derived compound that acts as a potent ghrelin receptor (GHS-R1a) antagonist (IC50 = 32nM in a binding assay, dissociation constant Kb = 19nM). Shown to reduce hexarelin-induced food intake [hexarelin (80ug/kg, cumulative food intake (g of food/100g of body weight) at 6h by acute administration (sc) of JMV 2959 (160ug/kg)] in rats without affecting the basal food intake. Also suppresses ghrelin and fasting-induced food intake at the level of the central nervous system. Reported to suppress genes up-regulated by ghrelin. Does not affect intracellular Ca2+ mobilization.
• Synonyms:(R)-N-(2-(1H-indol-3-yl)-1-(4-(4-methoxybenzyl)-5-phenethyl-4H-1,2,4-triazol-3-yl)ethyl)-2-aminoacetamide Hydrochloride, GHSR1a Antagonist, GH Secretagogue Receptor Antagonist, JMV2959, Growth Hormone Secretagogue Receptor Antagonist
• Molecular Formula:C₁₄H₁₄N₄O
• Molecular Weight:254.29
• Appearance:Supplied as a beige powder.
• Purity:~98% (HPLC)
• Primary Target:Ghrelin receptor
• Primary Target IC50:32nM
• Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.