Biochem/physiol Actions

Primary TargetGhrelin receptor

General description

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 K_b = 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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

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.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Physical form

Supplied as a hydrochloride salt.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)