345888

Ghrelin Receptor Antagonist, JMV 2959

• Synonym(s): Ghrelin Receptor Antagonist, JMV 2959, Growth hormone secretagogue receptor antagonist, (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
• Empirical Formula (Hill Notation): C₃₀H₃₂N₆O₂ · xHCl
• Molecular Weight: 508.61 (free base basis)
• UNSPSC Code: 12352200

Properties

• assay: ≥97% (HPLC)
• Quality Level: 100
• form: powder
• potency: 32 nM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: beige
• solubility: DMSO: 100 mg/mL; water: 5 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C

Description

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.

Biochem/physiol Actions

Primary Target
Ghrelin receptor

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

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.

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.

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable