4LSC3535 JMV2959 CAS# 925238-89-7

SKU: 4LSC3535 Category: Tag:

Catalog Number: 4LSC3535
CAS #: 925238-89-7
Name: JMV2959, (R)-N-(2-(1H-indol-3-yl)-1-(4-(4-methoxybenzyl)-5-phenethyl-4H-1,2,4-triazol-3-yl)ethyl)-2-aminoacetamide hydrochloride

JMV2959 is 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.

  • Molecular Formula: C30H33ClN6O2
  • Molecular Weight: 545.08 g/mol
  • Specification: Minimum purity: 95.0 %

The GHR-R antagonist JMV 2959 neither induces malaise nor alters the malaise property of LiCl in the https://doi.org/10.1371/journal.pone.0071284adult male rat. Juan A.Rodriguez et al., 2018, Physiology & Behavior, 183, 46-48. doi: 10.1016/j.physbeh.2017.10.017

 
Anorexigenic and electrophysiological actions of novel ghrelin receptor (GHS-R1A) antagonists in rats. N. Salome, et al., 2009, Eur. J. Pharmacol., 612 (1–3), 167-173.

doi: 10.1016/j.ejphar.2009.03.06610.1016

 

Ghrelin Receptor (GHS-R1A) Antagonism Suppresses Both Alcohol Consumption and the Alcohol Deprivation Effect in Rats following Long-Term Voluntary Alcohol Consumption. P. Suchankova et al., 2013, PLOS One, 8, 8, e7128. doi: 10.1371/journal.pone.0071284


You may also be interested in the following product: