345888

Ghrelin Receptor Antagonist, JMV 2959

• Synonyme(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
• Formule empirique (notation de Hill): C₃₀H₃₂N₆O₂ · xHCl
• Poids moléculaire : 508.61 (free base basis)
• Code UNSPSC : 12352200

Propriétés

• Pureté: ≥97% (HPLC)
• Niveau de qualité: 100
• Forme: powder
• Puissance: 32 nM IC₅₀
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: beige
• Solubilité: DMSO: 100 mg/mL; water: 5 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C

Description

Description générale

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.

Actions biochimiques/physiologiques

Primary Target
Ghrelin receptor

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Forme physique

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.

Autres remarques

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.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 2
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable