A 1, 2, 4-triazole derived compound that acts as a potent ghrelin receptor (GHS-R1a) antagonist (IC50 = 32 nM in a binding assay, dissociation constant Kb = 19 nM). Shown to reduce hexarelin-induced food intake [hexarelin (80 µg/kg, cumulative food intake (g of food/100 g of body weight) at 6 h by acute administration (sc) of JMV 2959 (160 µg/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.
10 mg in Glass bottle
Packaged under inert gas
Toxicity: Standard Handling (A)
Supplied as a hydrochloride salt.
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Moulin, A., et al. 2013. Amino Acids44, 301.
Mary, S., et al. 2012. Proc Natl Acad Sci USA109, 8304.
Salome, N., et al. 2009. Eur J Pharmacol.612, 167,.
Moulin, A., et al. 2007. J Med Chem50, 579.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany